JP/EN

INOUE
RESEARCH
GROUP

PUBLICATIONS

Masayuki Inoue

Original Papers

2024

J. Taguchi, S. Fukaya, H. Fujino, M. Inoue, "Total Synthesis of Euphorbialoid A," J. Am. Chem. Soc. 2024, 146, 34221-34230.
(24/12/12 Selected as Most Read Articles)
(Featured in Synfacts)
(Featured in Organic Chemistry Highlights)

DOI: 10.1021/jacs.4c14520
Y. Lin, H. Itoh, S. Dan,　M. Inoue, "Methyl scanning approach for enhancing the biological activity of the linear peptidic natural product, efrapeptin C," Chem. Sci. 2024, 15, 19390-19399.

DOI: 10.1039/D4SC04384G
T. Kato, K. Hagiwara, M. Inoue, "Generation and Coupling of Radical Species from α-Alkoxy Bridgehead Carboxylic Acid, Selenide, Telluride, Acyl Selenide, and Acyl Telluride," Chem. Pharm. Bull. 2024, 72, 767-771.

DOI: 10.1248/cpb.c24-00441
Y. Yamada, R. Yoshinaga, Y. Matsui, M. Nagatomo, H. Fujino, M. Inoue, "Et₃Al/Light-Promoted Radical-Polar Crossover Reactions of α-Alkoxyacyl Tellurides," J. Org. Chem. 2024, 89, 11701-11706.

DOI: 10.1021/acs.joc.4c01445
A. Watanabe, Y. Hikone, M. Nagatomo, M. Inoue, "Conversion of Phorbol into Des-D-Ring Tricycle and Crotonianoid B via Peroxidation Reaction," Org. Lett. 2024, 26, 4335-4339.

DOI: 10.1021/acs.orglett.4c01363
H. Mutoh, Y. Watanabe, D. Kamakura, K. Hagiwara, M. Inoue, "Unexpected Formation of 11(9→7)-abeo-Steroid Skeleton in Synthetic Studies toward Batrachotoxin," Chem. Pharm. Bull. 2024, 72, 360-364.

DOI: 10.1248/cpb.c24-00126
A. Watanabe, M. Nagatomo, A. Hirose, Y. Hikone, N. Kishimoto, S. Miura, T. Yasutake, T. Abe, S. Misumi, M. Inoue, "Total Syntheses of Phorbol and 11 Tigliane Diterpenoids and Their Evaluation as HIV Latency-Reversing Agents," J. Am. Chem. Soc. 2024, 146, 8746-8756.

DOI: 10.1021/jacs.4c01589
H. Asai, K. Hagiwara, M. Inoue, "Enantioselective route to an AE-ring intermediate in the total synthesis of talatisamine," Tetrahedron Lett. 2024, 135, 154903.

DOI: 10.1016/j.tetlet.2023.154903

2023

Y. Watanabe, K. Sakata, D. Urabe, K. Hagiwara, M. Inoue, "Formal Total Synthesis of Batrachotoxin Enabled by Radical and Weix Coupling Reactions," J. Org. Chem. 2023, 88, 17479-17484.
(24/1/4 Selected as Most Read Articles)

DOI: 10.1021/acs.joc.3c02290
T. Watanabe, K. Oga, H. Matoba, M. Nagatomo, M. Inoue, "Total Synthesis of Taxol Enabled by Intermolecular Radical Coupling and Pd-Catalyzed Cyclization," J. Am. Chem. Soc. 2023, 145, 25894.
(23/12/4 Selected as Most Read Articles)
(24/1/9 Featured in "Some Items of Interest to Process R&D Chemists and Engineers," Org. Process Res. Dev. 2024, 28, 1. )
(Featured in Synfacts)

DOI: 10.1021/jacs.3c10658
Y. Watanabe, H. Morozumi, H. Mutoh, K. Hagiwara, M. Inoue, "Total Synthesis of (−)-Batrachotoxin Enabled by a Pd/Ag-Promoted Suzuki–Miyaura Coupling Reaction," Angew. Chem. Int. Ed. 2023, 62, e202309688.
(Selected as Hot Paper)
(Selected as Top Viewed Article link)

DOI: 10.1002/anie.202309688
J. Fu, Y. Nakata, H. Itoh, S. Panthee, H. Hamamoto, K. Sekimizu, M. Inoue, "Molecular Editing Enhances Oxidation Resistance of Menaquinone-Targeting Antibiotics Lysocin E and WAP-8294A2," Chem. Eur. J. 2023, 29, e202301224.
DOI: 10.1002/chem.202301224
Y. Nakata, J. Fu, H. Itoh, S. Panthee, H. Hamamoto, K. Sekimizu, M. Inoue, "Construction of Five Tryptophan Isomers and Application of the Isomers to Solid-Phase Total Syntheses of Lysocin E Derivatives," Chem. Eur. J. 2023, 29, e202301225.
DOI: 10.1002/chem.202301225
H. Zhu, M. Kurokawa, M. Chen, Q. Wang, M. Inoue, T. Takao, "Characteristic Fragmentation of Polyunsaturated Fatty Acids with Allylic Vicinal Diols in Positive-Ion LC/ESI-MS/MS," J. Lipid Res. 2023, 64, 100384. DOI: 10.1016/j.jlr.2023.100384
Y.-W. Xue, K. Miura, H. Itoh, M. Inoue, "C-Terminal Modification of Polytheonamide B Uncouples Its Dual Functions in MCF-7 Cancer Cells," Chem. Commun. 2023, 59, 3914-3917.

DOI: 10.1039/D2CC05915K
Y. Imamura, K. Takaoka, Y. Komori, M. Nagatomo, M. Inoue, "Total Synthesis of Taxol Enabled by Inter- and Intramolecular Radical Coupling Reactions," Angew. Chem. Int. Ed. 2023, 62, e202219114.
(Selected as Hot Paper)
(Featured in Synfacts)
(Selected as Top Viewed Article link)

DOI: 10.1002/anie.202219114
T. Shimakawa, S. Nakamura, H. Asai, K. Hagiwara, M. Inoue, "Total Synthesis of Puberuline C," J. Am. Chem. Soc. 2023, 145, 600-609.
(Featured in ChemistryViews)
(Selected as Most Read Articles)
(Featured in Synfacts)
(Featured in Organic Chemistry Highlights)

DOI: 10.1021/jacs.2c11259

2022

N. Nakajima, E. Yoshida, T. Toma, Y. Nishiyama, M. Inoue, T. Fukuyama, S. Yokoshima, "Formal Synthesis of Ecteinascidin 743 via an Intramolecular Cascade Heck Reaction to Construct the Diazabicyclo[3.3.1]nonane Framework," Org. Lett. 2022, 22, 8228-8232.
DOI: 10.1021/acs.orglett.2c03357
Y.-W. Xue, H. Itoh, S. Dan, M. Inoue, "Gramicidin A Accumulates in Mitochondria, Reduces ATP Levels, Induces Mitophagy, and Inhibits Cancer Cell Growth," Chem. Sci. 2022, 13, 7482-7491.

DOI: 10.1039/D2SC02024F
T. Nagai, Y. Wang, K. Hagiwara, M. Inoue, "Asymmetric synthesis of evoninic acid," Tetrahedron Lett. 2022, 97, 153747.

DOI: 10.1016/j.tetlet.2022.153747
Y. Hikone, T. Kato, M. Nagatomo, M. Inoue, "Total Synthesis of Resiniferatoxin Enabled by Photocatalytic Decarboxylative Radical Cyclization," Org. Lett. 2022, 24, 929–933.
(Selected as Most Read Articles)

DOI: 10.1021/acs.orglett.1c04286
D. Kuwana, Y. Komori, M. Nagatomo, M. Inoue, "Photoinduced Decarboxylative Radical Coupling Reaction of Multiply Oxygenated Structures by Catalysis of Pt-Doped TiO₂," J. Org. Chem. 2022, 87, 730-736.

DOI: 10.1021/acs.joc.1c02736

2021

Y. Wang, T. Nagai, I. Watanabe, K. Hagiwara, M. Inoue, "Total Synthesis of Euonymine and Euonyminol Octaacetate," J. Am. Chem. Soc. 2021, 143, 21037–21047.
(Selected as Most Read Articles)

DOI: 10.1021/jacs.1c11038
H. Hamamoto, S. Panthee, A. Paudel, K. Ishii, J. Yasukawa, J. Su, A. Miyashita, H. Itoh, K. Tokumoto, M. Inoue, K. Sekimizu, "Serum apolipoprotein A-I potentiates the therapeutic efficacy of lysocin E against Staphylococcus aureus," Nat. Commun. 2021, 12, 6364.
DOI: 10.1038/s41467-021-26702-0
A. Hirose, A. Watanabe, K. Ogino, M. Nagatomo, M. Inoue, "Unified Total Syntheses of Rhamnofolane, Tigliane, and Daphnane Diterpenoids," J. Am. Chem. Soc. 2021, 143, 12387-12396.
(Featured in Synfacts)
(Highlighted in Organic Chemistry Highlights)

DOI: 10.1021/jacs.1c06450
A. Takeuchi, H. Itoh, M. Inoue, "¹⁸O/¹⁶O-Encoding Strategy for Microscale Stereochemical Determination of Peptidic Natural Products," Chem. Asian J. 2021, 16, 2447-2452.

DOI: 10.1002/asia.202100674
K. Kamiya, H. Itoh, M. Inoue, "Generation and Biological Evaluation of Degraded Derivatives of the Three E/Z-Isomers of Yaku'amide B," J. Nat. Prod. 2021, 84, 1854–1859.

DOI: 10.1021/acs.jnatprod.1c00339
H. Mutoh, S. Nakamura, K. Hagiwara, M. Inoue, "Construction of Pentacyclic Limonoid Skeletons via Radical Cascade Reactions," J. Org. Chem. 2021, 86, 6869–6878.

DOI: 10.1021/acs.joc.1c00212
K. Kamiya, K. Miura, H. Itoh, M. Inoue, "Divergent Solid‐Phase Synthesis and Biological Evaluation of Yaku’amide B and Its Seven E/Z Isomers," Chem. Eur. J. 2021, 27, 1088-1093.
(Selected as Hot Paper)

DOI: 10.1002/chem.202003858

2020

S. Shimizu, K. Hagiwara, H. Itoh, M. Inoue, "Unified Total Synthesis of Five Bufadienolides," Org. Lett. 2020, 22, 8652-8657.
(Selected as Most Read Articles of the month)

DOI: 10.1021/acs.orglett.0c03251
Y. Iwahashi, Y. Toyama, S. Imai, H. Itoh, M. Osawa, M. Inoue, I. Shimada, "Conformational equilibrium shift underlies altered K⁺ channel gating as revealed by NMR," Nat. Commun. 2020, 11, 5168.
DOI: 10.1038/s41467-020-19005-3
M. Nagatomo, K. Zhang, H. Fujino, M. Inoue, "Et3B/Et2AlCl/O2‐Mediated Radical Coupling Reaction between α‐Alkoxyacyl Tellurides and 2‐Hydroxybenzaldehyde Derivatives," Chem. Asian. J. 2020, 15, 3820-3824.

DOI: 10.1002/asia.202001090
Y. Takada, H. Itoh, A. Paudel, S. Panthee, H. Hamamoto, K. Sekimizu, M. Inoue, "Discovery of gramicidin A analogues with altered activities by multidimensional screening of a one-bead-one-compound library," Nat. Commun. 2020, 11, 4935.
(Highlighted in press releases of UTokyo FOCUS, link)
(Selected as Nature Communications Editors' Highlights, link)

DOI: 10.1038/s41467-020-18711-2
T. Teratani, Y. Mikami, N. Nakamoto, T. Suzuki, Y. Harada, K. Okabayashi, Y. Hagihara, N. Taniki, K. Kohno, S. Shibata, K. Miyamoto, H. Ishigame, P.-S. Chu, T. Sujino, W. Suda, M. Hattori, M. Matsui, T. Okada, H. Okano, M. Inoue, T. Yada, Y. Kitagawa, A. Yoshimura, M. Tanida, M. Tsuda, Y. Iwasaki, T. Kanai, "The Liver-Brain-Gut Neural Arc Maintains the Treg Cell Niche in the Gut," Nature 2020, 585, 591-596.
DOI: 10.1038/s41586-020-2425-3
T. Fukuda, M. Nagatomo, M. Inoue, "Total Synthesis of Diospyrodin and Its Three Diastereomers," Org. Lett. 2020, 22, 6468–6472.

DOI: 10.1021/acs.orglett.0c02280
K. Minagawa, D. Kamakura, K. Hagiwara, M. Inoue, "Construction of the ABCE-ring structure of talatisamine via decarboxylative radical cyclization," Tetrahedron 2020, 76, 131385.
(Selected in Editor’s Choice Collection, link)

DOI: 10.1016/j.tet.2020.131385
H. Fujino, T. Fukuda, M. Nagatomo, M. Inoue, "Convergent Total Synthesis of Hikizimycin Enabled by Intermolecular Radical Addition to Aldehyde," J. Am. Chem. Soc. 2020, 142, 13227–13234.
(Highlighted in Organic Chemistry Highlights)

DOI: 10.1021/jacs.0c06354
J. Mao, H. Itoh, K. Sakurai, M. Inoue, "Phospholipid-Dependent Functions of a Macrocyclic Analogue of the Ion-Channel-Forming Antibiotic Gramicidin A," Chem. Pharm. Bull. 2020, 68, 173-178.

DOI: 10.1248/cpb.c19-00967
H. Itoh, K. Miura, K. Kamiya, T. Yamashita, M. Inoue, "Solid‐Phase Total Synthesis of Yaku’amide B Enabled by Traceless Staudinger Ligation," Angew. Chem. Int. Ed. 2020, 59, 4564-4571.

DOI: 10.1002/anie.201916517
D. Kamakura, H. Todoroki, D. Urabe, K. Hagiwara, M. Inoue, "Total Synthesis of Talatisamine," Angew. Chem. Int. Ed. 2020, 59, 479-486.
(Featured in Synfacts)
(Featured in Synthesis Workshop Videos, link)
(Selected as Top Downloaded Article link)

DOI: 10.1002/anie.201912737

2019

Y.-W. Xue, A. Hayata, H. Itoh, M. Inoue, "Biological Effects of a Simplified Synthetic Analogue of Ion‐Channel‐Forming Polytheonamide B on Plasma Membrane and Lysosomes," Chem. Eur. J. 2019, 25, 15198-15204.
(Selected as Hot Paper)

DOI: 10.1002/chem.201903974
E. O. Balogun, D. K. Inaoka, T. Shiba, C. Tsuge, B. May, T. Sato, Y. Kido, T. Nara, T. Aoki, T. Honma, A. Tanaka, M. Inoue, S. Matsuoka, P. A. M. Michels, Y.-I. Watanabe, A. L. Moore, S. Harada, K. Kita, "Discovery of Trypanocidal Coumarins with Dual Inhibition of Both the Glycerol Kinase and Alternative Oxidase of Trypanosoma brucei brucei," FASEB J. 2019, 33, 13002-13013.
DOI: 10.1096/fj.201901342R
D. Kuwana, M. Nagatomo, M. Inoue, "Total Synthesis of 5-epi-Eudesm-4(15)-ene-1β,6β-diol via Decarbonylative Radical Coupling Reaction," Org. Lett. 2019, 21, 7619-7623.

DOI: 10.1021/acs.orglett.9b02895
H. Itoh, K. Tokumoto, T. Kaji, A. Paudel, S. Panthee, H. Hamamoto, K. Sekimizu, M. Inoue, "Development of a high-throughput strategy for discovery of potent analogues of antibiotic lysocin E," Nat. Commun. 2019, 10, 2992.
(Highlighted in press releases of UTokyo FOCUS, link)
(Selected as Nature Communications Editor's Highlights. link)

DOI: 10.1038/s41467-019-10754-4
Y. Imamura, S. Yoshioka, M. Nagatomo, M. Inoue, "Total Synthesis of 1‐Hydroxytaxinine," Angew. Chem. Int. Ed. 2019, 58, 12159-12163.
(Selected as Hot Paper)
(Highlighted in Organic Chemistry Highlights)

DOI: 10.1002/anie.201906872
D. Kuwana, B. Ovadia, D. Kamimura, M. Nagatomo, M. Inoue, "Installation of O‐Heterocycles to N‐Heteroarenes via an Et₃B/O₂‐mediated Radical Reaction of α-Alkoxy and α-Alkoxyacyl Tellurides," Asian J. Org. Chem. 2019, 8, 1088-1091.

DOI: 10.1002/ajoc.201900170
T. Shiba, D. K. Inaoka, G. Takahashi, C. Tsuge, Y. Kido, L. Young, S. Ueda, E. O. Balogun, T. Nara, T. Honma, A. Tanaka, M. Inoue, H. Saimoto, S. Harada, A. L. Moore, K. Kita, "Insights into the Ubiquinol/dioxygen Binding and Proton Relay Pathways of the Alternative Oxidase," Biochim. Biophys. Acta, Bioenerg. 2019, 1860, 375-382.
DOI: 10.1016/j.bbabio.2019.03.008
M. Nagatomo, Y. Fujimoto, K. Masuda, M. Inoue, "Construction of a 6/5/9-membered tricyclic structure of cladiellins via radical-polar crossover reaction," J. Antibiot. 2019, 72, 486-489.
DOI: 10.1038/s41429-019-0150-7

2018

H. Matoba, T. Watanabe, M. Nagatomo, M. Inoue, "Convergent Synthesis of Taxol Skeleton via Decarbonylative Radical Coupling Reaction," Org. Lett. 2018, 20, 7554-7557.
(Selected as Most Read Articles of the month)

DOI: 10.1021/acs.orglett.8b03302
T. Kawamata, A. Yamaguchi, M. Nagatomo, M. Inoue, "Convergent Total Synthesis of Asimicin via Decarbonylative Radical Dimerization," Chem. Eur. J. 2018, 24, 18907-18912.
DOI: 10.1002/chem.201805317
D. Urabe, Y. Nakagawa, K. Mukai, K. Fukushima, N. Aoki, H. Itoh, M. Nagatomo, M. Inoue, "Total synthesis and biological evaluation of 19-hydroxysarmentogenin-3-O-a-L-rhamnoside, trewianin, and their aglycons," J. Org. Chem. 2018, 83, 13888-13910.

DOI: 10.1021/acs.joc.8b02219
K. Kitamura, H. Itoh, K. Sakurai, S. Dan, M. Inoue, "Target Identification of Yaku’amide B and Its Two Distinct Activities against Mitochondrial FoF1-ATP Synthase," J. Am. Chem. Soc. 2018, 140, 12189-12199.
(Selected as Spotlights on Recent JACS Publications)

DOI: 10.1021/jacs.8b07339
A. Hayata, H. Itoh, M. Inoue, "Solid-Phase Total Synthesis and Dual Mechanism of Action of the Channel-Forming 48-mer Peptide Polytheonamide B," J. Am. Chem. Soc. 2018, 140, 10602-10611.

DOI: 10.1021/jacs.8b06755
M. Koshimizu, M. Nagatomo, M. Inoue, "Construction of a pentacyclic ring system of isoryanodane diterpenoids by SmI₂-mediated transannular cyclization," Tetrahedron 2018, 74, 3384-3390.

DOI: 10.1016/j.tet.2018.03.061
Y. Kofuku, T. Yokomizo, S. Imai, Y. Shiraishi, M. Natsume, H. Itoh, M. Inoue, K. Nakata, S. Igarashi, H. Yamaguchi, T. Mizukoshi, E. Suzuki, T. Ueda, I. Shimada, "Deuteration and selective labeling of alanine methyl groups of β₂-adrenergic receptor expressed in a baculovirus-insect cell expression system," J. Biomol. NMR 2018, 71, 185-192.
DOI: 10.1007/s10858-018-0174-5
K. Sakata, Y. Wang, D. Urabe, M. Inoue, "Synthesis of the Tetracyclic Structure of Batrachotoxin Enabled by Bridgehead Radical Coupling and Pd/Ni-Promoted Ullmann Reaction," Org. Lett. 2018, 20, 130-133.

DOI: 10.1021/acs.orglett.7b03482
T. Mochimaru, K. Fukunaga, J. Miyata, M. Matsusaka, K. Masaki, H. Kabata, S. Ueda, Y. Suzuki, T. Goto, D. Urabe, M. Inoue, Y. Isobe, M. Arita, T. Betsu, "12-OH-17,18-Epoxyeicosatetraenoic acid alleviates eosinophilic airway inflammation in murine lungs," Allergy 2018, 73, 369-378.
DOI: 10.1111/all.13297
K. Minagawa, D. Urabe, M. Inoue, "A three-component coupling approach to the ACE-ring substructure of C19-diterpene alkaloids," J. Antibiotics 2018, 71, 326-332.
DOI: 10.1038/ja.2017.69
H. Itoh, K. Tokumoto, T. Kaji, A. Paudel, S. Panthee, H. Hamamoto, K. Sekimizu, M. Inoue, "Total Synthesis and Biological Mode of Action of WAP-8294A2: A Menaquinone-Targeting Antibiotic," J. Org. Chem. 2018, 83, 6924-6935.
(Selected as ACS editors' choice)
(The Journal of Organic Chemistry Outstanding Publication of the Year Lectureship Award)
(Selected as the three most read papers in JOC in 2018)

DOI:10.1021/acs.joc.7b02318

2017

S. Hashimoto, S. Katoh, T. Kato, D. Urabe, M. Inoue, "Total Synthesis of Resiniferatoxin Enabled by Radical-Mediated Three-Component Coupling and 7-endo Cyclization," J. Am. Chem. Soc. 2017, 139, 16420-16429.

DOI: 10.1021/jacs.7b10177
H. Fujino, M. Nagatomo, A. Paudel, S. Panthee, H. Hamamoto, K. Sekimizu, M. Inoue, "Unified Total Synthesis of Polyoxin J, L, and Their Fluorinated Analogues on the Basis of Decarbonylative Radical Coupling Reactions," Angew. Chem. Int. Ed. 2017, 56, 11865-11869.

DOI:10.1002/anie.201706671
H. Umihara, S. Yokoshima, M. Inoue, T. Fukuyama, "Total Synthesis of (-)-Morphine," Chem. Eur. J. 2017, 23, 6993-6995.

DOI:10.1002/chem.201701438
K. Masuda, M. Tanigawa, M. Nagatomo, D. Urabe, M. Inoue, "Construction of carbocycles initiated by Cu-catalyzed radical reaction of Cl₂C(CN)₂," Tetrahedron 2017, 73, 3596-3605.

DOI:10.1016/j.tet.2017.03.063
H. Fujisawa, T. Ishiyama, D. Urabe, M. Inoue, "Construction of the septahydroxylated ABC-ring system of dihydro-β-agarofurans: Application of 6-exo-dig radical cyclization," Chem. Commun. 2017, 53, 4073-4076.

DOI:10.1039/C7CC00507E
T. Kawamata, M. Nagatomo, M. Inoue, "Total Synthesis of Zaragozic Acid C: Implementation of Photochemical C(sp³)-H Acylation," J. Am. Chem. Soc. 2017, 139, 1814-1817.
(Highlighted in Synfacts 2017, 13, 0337. and selected as its Cover Picture)

DOI:10.1021/jacs.6b13263
D. K. Inaoka, M. Iida, S. Hashimoto, T. Tabuchi,T. Kuranaga, E. O. Balogun, T. Honma, A. Tanaka, S. Harada, T. Nara, K. Kita, M. Inoue, "Design and Synthesis of Potent Substrate-based Inhibitors of the Trypanosoma cruzi Dihydroorotate Dehydrogenase," Bioorg. Med. Chem. 2017, 25, 1465-1470.

DOI:10.1016/j.bmc.2017.01.009
K. Masuda, M. Nagatomo, M. Inoue, "Direct assembly of multiply oxygenated carbon chains by decarbonylative radical-radical coupling reactions," Nature Chem. 2017, 9, 207-212.
(Highlighted in Synfacts 2017, 13, 0534.)
(Associated Link: News and Views - "Organic chemistry: A radical step forward")

DOI:10.1038/nchem.2639

2016

D. K. Inaoka, M. Iida, T. Tabuchi, T. Honma, N. Lee, S. Hashimoto, S. Matsuoka, T. Kuranaga, K. Sato, T. Shiba, K. Sakamoto, E. O. Balogun, S. Suzuki, T. Nara, J. R. Rocha, C. A. Montanari, A. Tanaka, M. Inoue, K. Kita, S. Harada, "The Open Form Inducer Approach for Structure-Based Drug Design," PLoS ONE 2016, 11, e0167078.
DOI:10.1371/journal.pone.0167078
T. Kaji, M. Murai, H. Itoh, J. Yasukawa, H. Hamamoto, K. Sekimizu, M. Inoue, "Total Synthesis and Functional Evaluation of Fourteen Derivatives of Lysocin E: Importance of Cationic, Hydrophobic, and Aromatic Moieties for Antibacterial Activity," Chem. Eur. J. 2016, 22, 16912-16919.

DOI:10.1002/chem.201604022
S. Matsumura, Y. Matsui, M. Nagatomo, M. Inoue, "Stereoselective construction of anti- and syn-1,2-diol structures via decarbonylative radical coupling of α-alkoxyacyl tellurides," Tetrahedron 2016, 72, 4859-4866.

DOI:10.1016/j.tet.2016.06.056
T. Tabuchi, D. Urabe, M. Inoue, "Construction of the Fused Pentacycle of Talatisamine via a Combination of Radical and Cationic Cyclizations," J. Org. Chem. 2016, 81, 10204-10213.

DOI:10.1021/acs.joc.6b01011
D. Kamimura, M. Nagatomo, D. Urabe, M. Inoue, "Expanding the scope of Et₃B/O₂-mediated coupling reactions of O,Te-acetal," Tetrahedron 2016, 72, 7839-7848.

DOI:10.1016/j.tet.2016.04.023
H. Mutoh, Y. Sesoko, T. Kuranaga, H. Itoh, M. Inoue, "Total Synthesis and Functional Evaluation of Fourteen Stereoisomers of Yaku’amide B. Importance of Stereochemistry for Hydrophobicity and Cytotoxicity," Org. Biomol. Chem. 2016, 14, 4199-4204.
(Selected as Hot Article)
(Selected as 2016's Most Popular Article)

DOI: 10.1039/C6OB00640J
K. Masuda, M. Nagatomo, M. Inoue, "Chemical Conversion of Ryanodol to Ryanodine," Chem. Pharm. Bull. 2016, 64, 874-879.

DOI: 10.1248/cpb.c16-00214
K. Hagiwara, T. Tabuchi, D. Urabe, M. Inoue, "Expeditious synthesis of the fused hexacycle of puberuline C via radical-based cyclization/translocation/cyclization process," Chem. Sci. 2016, 7, 4372-4378.

DOI: 10.1039/C6SC00671J
F. Zhao, X. Li, L. Jin, F. Zhang, M. Inoue, B. Yu, Z. Cao, "Development of a Rapid Throughput Assay for Identification of hNav1.7 Antagonist Using Unique Efficacious Sodium Channel Agonist, Antillatoxin," Mar. Drugs. 2016, 14, 36-47.
DOI: 10.3390/md14020036
A. Hayata, H. Itoh, S. Matsutaka, M. Inoue, "Dual Chemical Modification of a Polytheonamide Mimic: Rational Design and Synthesis of Ion-Channel-Forming 48-mer Peptides with Potent Cytotoxicity," Chem. Eur. J. 2016, 22, 3370-3377.
(Selected as Very Important Paper)

DOI: 10.1002/chem.201504632
M. Koshimizu, M. Nagatomo, M. Inoue, "Unified Total Synthesis of 3-epi-Ryanodol, Cinnzeylanol, Cinncassiols A and B, and Structural Revision of Natural Ryanodol and Cinnacasol," Angew. Chem. Int. Ed. 2016, 55, 2493-2497.

DOI: 10.1002/anie.201511116
K. Masuda, M. Koshimizu, M. Nagatomo, M. Inoue, "Asymmetric Total Synthesis of (+)-Ryanodol and (+)-Ryanodine," Chem. Eur. J. 2016, 22, 230-236.

DOI: 10.1002/chem.201503641
M. Nagatomo, K. Hagiwara, K. Masuda, M. Koshimizu, T. Kawamata, Y. Matsui, D. Urabe, M. Inoue, " Symmetry-Driven Strategy for the Assembly of the Core Tetracycle of (+)-Ryanodine: Synthetic Utility of a Cobalt-Catalyzed Olefin Oxidation and α-Alkoxy Bridgehead Radical Reaction," Chem. Eur. J. 2016, 22, 222-229.

DOI: 10.1002/chem.201503640

2015

J. Okude, T. Ueda,Y. Kofuku, M. Sato,N. Nobuyama, K. Kondo, Y. Shiraishi, T. Mizumura, K. Onishi, M. Natsume, M. Maeda, H. Tsujishita, T. Kuranaga, M. Inoue, I. Shimada, "Identification of a Conformational Equilibrium That Determines the Efficacy and Functional Selectivity of the μ-Opioid Receptor," Angew. Chem. Int. Ed. 2015, 54, 15771-15776.

DOI: 10.1002/anie.201508794
T. Asaba, Y. Katoh, D. Urabe, M. Inoue, "Total Synthesis of Crotophorbolone," Angew. Chem. Int. Ed. 2015, 54, 14457-14461.
(Highlighted in Synfacts 2016, 12, 0002. )

DOI: 10.1002/anie.201509160
T. Goto, D. Urabe, Y. Isobe, M. Arita, M. Inoue, "Total Synthesis of Four Stereoisomers of (5Z,8Z,10E,14Z)-12-Hydroxy-17,18-epoxy-5,8,10,14-eicosatetraenoic Acid and Their Anti-Inflammatory Activities," Tetrahedron 2015, 71, 8320-8332.

DOI: 10.1016/j.tet.2015.08.047
T. Goto, D. Urabe, K. Masuda, Y. Isobe, M. Arita, M. Inoue, "Total Synthesis of Four Stereoisomers of (4Z,7Z,10Z,12E,16Z,18E)-14,20-Dihydroxy-4,7,10,12,16,18-docosahexaenoic Acid and Their Anti-inflammatory Activities," J. Org. Chem. 2015, 80, 7713-7726.

DOI: 10.1021/acs.joc.5b01461
T. Kuranaga, H. Mutoh, Y. Sesoko, T. Goto, S. Matsunaga, M. Inoue, "Elucidation and Total Synthesis of the Correct Structures of Tridecapeptides Yaku’amides A and B. Synthesis-Driven Stereochemical Reassignment of Four Amino Acid Residues," J. Am. Chem. Soc. 2015, 137, 9443-9451.

DOI: 10.1021/jacs.5b05550
D. K. Inaoka, T. Shiba, D. Sato, E. O. Balogun,T. Sasaki, M. Nagahama, M. Oda, S. Matsuoka, J. Ohmori, T. Honma, M. Inoue, K. Kita, S. Harada, "Structural Insights into the Molecular Design of Flutolanil Derivatives Targeted for Fumarate Respiration of Parasite Mitochondria," Int. J. Mol. Sci. 2015, 16, 15287-15308.

DOI: 10.3390/ijms160715287
R. Yoshino, N. Yasuo, D. K. Inaoka, Y. Hagiwara, K. Ohno, M. Orita, M. Inoue, T. Shiba, S. Harada, T. Honma, E. O. Balogun, J. Rodrigues da Rocha, C. A. Montanari, K. Kita, M. Sekijima, "Pharmacophore Modeling for Anti-Chagas Drug Design Using the Fragment Molecular Orbital Method," PLoS ONE 2015, 10, e0125829.
DOI: 10.1371/journal.pone.0125829
T. Yamashita, T. Kuranaga, M. Inoue, "Solid-Phase Total Synthesis of Bogorol A: Stereocontrolled Construction of Thermodynamically Unfavored (E)-2-Amino-2-butenamide," Org. Lett. 2015, 17, 2170-2173.

DOI: 10.1021/acs.orglett.5b00769
K. Mukai, S. Kasuya, Y. Nakagawa, D. Urabe, M. Inoue, "A Convergent Total Synthesis of Ouabagenin," Chem. Sci. 2015, 6, 3383-3387.

DOI: 10.1039/C5SC00212E
M. Nagatomo, D. Kamimura, Y. Matsui, K. Masuda, M. Inoue, "Et₃B-Mediated Two- and Three-Component Coupling Reactions via Radical Decarbonylation of α-Alkoxyacyl Tellurides: Single-Step Construction of Densely Oxygenated Carboskeletons," Chem. Sci. 2015, 6, 2765-2769.

DOI: 10.1039/C5SC00457H
S. Yamashita, K. Takeuchi, T. Koyama, M. Inoue, Y. Hayashi, M. Hirama, "Practical Route to the Left Wing of CTX1B and Total Syntheses of CTX1B and 54-deoxyCTX1B," Chem. Eur. J. 2015, 21, 2621-2628.

DOI: 10.1002/chem.201405629
S. Yoshioka, M. Nagatomo, M. Inoue, "Application of Two Direct C(sp³)-H Functionalizations for Total Synthesis of (+)-Lactacystin," Org. Lett. 2015, 17, 90-93.

DOI: 10.1021/ol503291s
J. Mao, T. Kuranaga, H. Hamamoto, K. Sekimizu, M. Inoue, "Rational Design, Synthesis, and Biological Evaluation of Lactam-Bridged Gramicidin A Analogues: Discovery of a Low-Hemolytic Antibacterial Peptide," ChemMedChem. 2015, 10, 540-545.

DOI: 10.1002/cmdc.201402473
M. Murai, T. Kaji, T. Kuranaga, H. Hamamoto, K. Sekimizu, M. Inoue, "Total Synthesis and Biological Evaluation of the Antibiotic Lysocin E and Its Enantiomeric, Epimeric, and N-Demethylated Analogues," Angew. Chem. Int. Ed. 2015, 54, 1556-1560.

DOI: 10.1002/anie.201410270
M. Nagatomo, H. Nishiyama, H. Fujino, M. Inoue, "Decarbonylative Radical Coupling of α-Aminoacyl Tellurides: Single-Step Preparation of γ-Amino and α,β-Diamino Acids and Rapid Synthesis of Gabapentin and Manzacidin A," Angew. Chem. Int. Ed. 2015, 54, 1537-1541.
(Selected as Hot Paper)

DOI: 10.1002/anie.201410186
H. Hamamoto, M. Urai, K. Ishii, J. Yasukawa, A. Paudel, M. Murai, T. Kaji, T. Kuranaga, K. Hamase, T. Katsu, J. Su, T. Adachi, R. Uchida, H. Tomoda, M. Yamada, M. Souma, H. Kirihara, M. Inoue, K. Sekimizu, "Lysocin E is a new antibiotic that targets menaquinone in the bacterial membrane," Nat. Chem. Biol. 2015, 11, 127-133.

DOI: 10.1038/nchembio.1710
M. Nagatomo, S. Yoshioka, M. Inoue, "Enantioselective Radical Alkynylation of C(sp³)-H Bonds Using Sulfoximine as a Traceless Chiral Auxiliary," Chem. Asian. J. 2015, 10, 120-123.

DOI: 10.1002/asia.201402983
K. Hagiwara, M. Iwatsu, D. Urabe, M. Inoue, "N-(2,3,4,5,6-Pentafluorophenyl)maleimide as a Powerful Dienophile in Dearomatizing Diels-Alder Reactions," Heterocycles 2015, 90, 659-672.

DOI: 10.3987/COM-14-S(K)23

2014

Y. Yokokura, Y. Isobe, S. Matsueda, R. Iwamoto, T. Goto, T. Yoshioka, D. Urabe, M. Inoue, H. Arai, M. Arita, "Identification of 14,20-dihydroxy-docosahexaenoic acid as a novel anti-inflammatory metabolite," J. Biochem. 2014, 156, 315-321.
DOI: 10.1093/jb/mvu044
E. O. Balogun, D. K. Inaoka, T. Shiba, Y. Kido, C. Tsuge, T. Nara, T. Aoki, T. Honma, A. Tanaka, M. Inoue, S. Matsuoka, P. A. M. Michels, K. Kita, S. Harada, "Molecular Basis for the Reverse Reaction of African Human Trypanosomes Glycerol Kinase," Mol. Microbiol. 2014, 94, 1315-1329.
DOI: 10.1111/mmi.12831
H. Todoroki, M. Iwatsu, D. Urabe, M. Inoue, "Total Synthesis of (－)-4-Hydroxyzinowol," J. Org. Chem. 2014, 79, 8835-8849.

DOI: 10.1021/jo501666x
Y. Amaoka, M. Nagatomo, M. Watanabe, K. Tao, S. Kamijo, M. Inoue, "Photochemically Induced Radical Alkenylation of C(sp³)-H Bonds," Chem. Sci. 2014, 5, 4339-4345.

DOI: 10.1039/C4SC01631A
T. Yamashita, H. Matoba, T. Kuranaga, M. Inoue, "Total syntheses of nobilamides B and D: application of traceless Staudinger ligation," Tetrahedron 2014, 70, 7746-7752.

DOI: 10.1016/j.tet.2014.05.091
K. Hagiwara, D. Urabe, M. Inoue, "Studies in symmetry-driven synthesis of ryanodol: application of nucleophilic alkynylation for regio- and stereoselective desymmetrization," Tetrahedron Lett. 2014, 55, 3817.

DOI: 10.1016/j.tetlet.2014.05.075
M. Nagatomo, M. Koshimizu, K. Masuda, T. Tabuchi, D. Urabe, M. Inoue, "Total Synthesis of Ryanodol," J. Am. Chem. Soc. 2014, 136, 5916-5919.

DOI: 10.1021/ja502770n
T. Kubota, M. Arita, Y. Isobe, R. Iwamoto, T. Goto, T. Yoshioka, D. Urabe, M. Inoue, H. Arai, "Eicosapentaenoic Acid Is Converted via ω-3 Epoxygenation to the Anti-inflammatory Metabolite 12-Hydroxy-17,18-epoxyeicosatetraenoic acid," FASEB J. 2014, 28, 586-593.
DOI: 10.1096/fj.13-236224
H. Itoh, S. Matsutaka, T. Kuranaga, M. Inoue, "Control of the cytotoxicity of dansylated polytheonamide mimic, an artificial peptide ion channel, by modification of the N-terminal structure," Tetrahedron Lett. 2014, 55, 728-731.

DOI: 10.1016/j.tetlet.2013.12.007
H. Itoh, M. Inoue, "Antibody-mediated functional control of a dansylated polytheonamide mimic," Chem. Commun. 2014, 50, 939-941.

DOI: 10.1039/C3CC48348G

2013

D. Kamimura, D. Urabe, M. Nagatomo, M. Inoue, "Et₃B‐Mediated Radical-Polar Crossover Reaction for Single-Step Coupling of O,Te-Acetal, α,β-Unsaturated Ketones, and Aldehydes/Ketones," Org. Lett. 2013, 15, 5122-5125.

DOI: 10.1021/ol402563v
T. Ishiyama, D. Urabe, H. Fujisawa, M. Inoue, "Concise Synthesis of the Multiply Oxygenated ABC-Ring System of the Dihydro-β-agarofurans," Org. Lett. 2013, 15, 4488-4491.

DOI: 10.1021/ol402038b
K. Okura, M. Inoue, "The Orientation of the Terminal tBu Group of Antillatoxin is Important for Potent Toxicity: Design, Synthesis and Biological Evaluation of Conformationally Restricted Analogues of Antillatoxin," Asian J. Org. Chem. 2013, 2, 650-653.

DOI: 10.1002/ajoc.201300111
K. Okura, S. Matsuoka, M. Inoue, "The bulky side chain of antillatoxin is important for potent toxicity: rational design of photoresponsive cytotoxins based on SAR studies," Chem. Commun. 2013, 49, 8024-8026.

DOI: 10.1039/C3CC44066D
K. Sakata, D. Urabe, M. Inoue, "Preparation and palladium-mediated cross-coupling of α-benzoyloxyalkylzinc bromides," Tetrahedron Lett. 2013, 54, 4189-4192.

DOI: 10.1016/j.tetlet.2013.05.114
T. Hoshikawa, M. Inoue, "Photoinduced Direct 4-Pyridination of C(sp³)-H Bonds," Chem. Sci. 2013, 4, 3118-3123.

DOI: 10.1039/C3SC51080H
Y. Amaoka, M. Nagatomo, M. Inoue, "Metal-Free Fluorination of C(sp³)-H Bonds Using a Catalytic N-Oxyl Radical," Org. Lett. 2013, 15, 2160-2163.

DOI: 10.1021/ol4006757
K. Mukai, D. Urabe, S. Kasuya, N. Aoki, M. Inoue, "A Convergent Total Synthesis of 19-Hydroxysarmentogenin," Angew. Chem. Int. Ed. 2013, 52, 5300-5304.

DOI: 10.1002/anie.201302067
T. Kuranaga, Y. Sesoko, K. Sakata, N. Maeda, A. Hayata, M. Inoue, "Total Synthesis and Complete Structural Assignment of Yaku’amide A," J. Am. Chem. Soc. 2013, 135, 5467-5474.

DOI: 10.1021/ja401457h
K. Murai, S. Katoh, D. Urabe, M. Inoue, "A radical-based approach for the construction of the tetracyclic structure of resiniferatoxin," Chem. Sci. 2013, 4, 2364-2368.

DOI: 10.1039/C3SC50329A
T. Tabuchi, D. Urabe, M. Inoue, "Asymmetric synthesis of a highly functionalized bicyclo[3.2.2]nonene derivative," Beilstein J. Org. Chem. 2013, 9, 655-663.

DOI: 10.3762/bjoc.9.74
E. O. Balogun, D. K. Inaoka, T. Shiba, Y. Kido, T. Nara, T. Aoki, T. Honma, A. Tanaka, M. Inoue, S. Matsuoka, P. AM. Michels, S. Harada, K. Kita, "Biochemical characterization of highly active Trypanosoma brucei gambiense glycerol kinase, a promising drug target," J. Biochem. 2013, 154, 77-84.
DOI: 10.1093/jb/mvt037
T. Shiba, Y. Kido, K. Sakamoto, D. K. Inaoka, C. Tsuge, R. Tatsumi, G. Takahashi, E. O. Balogun, T. Nara, T. Aoki, T. Honma, A. Tanaka, M. Inoue, S. Matsuoka, H. Saimoto, A. L. Moore, S. Harada, K. Kita, "Structure of the Trypanosome Cyanide-insensitive Alternative Oxidase, a Promising Drug Target," Proc. Natl. Acad. Sci. U.S.A. 2013, 110, 4580-4585.
DOI: 10.1073/pnas.1218386110
T. Hoshikawa, S. Yoshioka, S. Kamijo, M. Inoue, "Photoinduced Direct Cyanation of C(sp³)-H Bonds," Synthesis 2013, 45, 874-887.

DOI: 10.1055/s-0032-1318325
D. Urabe, M. Nagatomo, K. Hagiwara, K. Masuda, M. Inoue, "Symmetry-Driven Synthesis of 9-Demethyl-10,15-dideoxyryanodol," Chem. Sci. 2013, 4, 1615-1619.

DOI: 10.1039/C3SC00023K
Y. Isobe, M. Arita, R. Iwamoto, D. Urabe, H. Todoroki, K. Masuda, M. Inoueand H. Arai, "Stereochemical assignment and anti-inflammatory properties of the omega-3 lipid mediator resolvin E3," J. Biochem. 2013, 153, 355-360.
DOI: 10.1093/jb/mvs151
H. Itoh, M. Inoue, "Structural Permutation of Potent Cytotoxin, Polytheonamide B: Discovery of Cytotoxic Peptide with Altered Activity," ACS Med. Chem. Lett. 2013, 4, 52-56.

DOI: 10.1021/ml300264c
T. Hoshikawa, S. Kamijo, M. Inoue, "Photochemically Induced Radical Alkynylation of C(sp³)-H Bonds," Org. Biomol. Chem. 2013, 11, 164-169.

DOI: 10.1039/C2OB26785C

2012

Y. Amaoka, S. Kamijo, T. Hoshikawa, M. Inoue, "Radical Amination of C(sp³)-H Bonds Using N-Hydroxyphthalimide and Dialkyl Azodicarboxylate," J. Org. Chem. 2012, 77, 9959-9969.

DOI: 10.1021/jo301840e
H. Itoh, S. Matsuoka, M. Kreir, M. Inoue, "Design, Synthesis and Functional Analysis of Dansylated Polytheonamide Mimic: An Artificial Peptide Ion Channel," J. Am. Chem. Soc. 2012, 134, 14011-14018.

DOI: 10.1021/ja303831a
M. Iwatsu, D. Urabe, H. Todoroki, K. Masuda, M. Inoue, "Selective Introduction of Four Contiguous Stereocenters on the B-Ring of 4-Hydroxyzinowol," Heterocycles 2012, 86, 181-188.

DOI: 10.3987/COM-12-S(N)76
D. Urabe, H. Yamaguchi, A. Someya, M. Inoue, "Intermolecular Radical Reaction of O,Se-Acetals Generated via Seleno-Pummerer Rearrangement," Org. Lett. 2012, 14, 3842-3845.

DOI: 10.1021/ol301482f
S. Kamijo, S. Matsumura, M. Inoue, "Microwave-assisted atom transfer radical addition of polychlorinated compounds to olefins without addition of metal catalysts," Tetrahedron Lett. 2012, 53, 4368-4371.

DOI: 10.1016/j.tetlet.2012.06.027
S. Kamijo, S. Yokosaka, M. Inoue, "Carbocyanation of trisubstituted olefins via Cu-catalyzed atom transfer radical addition," Tetrahedron Lett. 2012, 53, 4324-4327.

DOI: 10.1016/j.tetlet.2012.06.004
N. Shinohara, H. Itoh, S. Matsuoka, M. Inoue, "Selective Modification of the N-Terminal Structure of Polytheonamide B Significantly Changes its Cytotoxicity and Activity as an Ion Channel," ChemMedChem 2012, 7, 1770-1773.

DOI: 10.1002/cmdc.201200142
T. Nara, M. Hashimoto, H. Hirawake, C.-W. Liao, Y. Fukai, S. Suzuki, A. Tsubouchi, J. Morales, S. Takamiya, T. Fujimura, H. Taka, R. Mineki, C.-K. Fan, D. K. Inaoka, M. Inoue, A. Tanaka, S. Harada, K. Kita, T. Aoki, "Molecular Interaction of the First 3 Enzymes of the De Novo Pyrimidine Biosynthetic Pathway of Trypanosoma Cruzi," Biochem. Biophys. Res. Commun. 2012, 418, 140-143.
DOI: 10.1016/j.bbrc.2011.12.148
M. Hashimoto, J. Morales, Y. Fukai, S. Suzuki, S. Takamiya, A. Tsubouchi, S. Inoue, M. Inoue, K. Kita, S. Harada, A. Tanaka, T. Aoki, T. Nara, "Critical Importance of the De Novo Pyrimidine Biosynthesis Pathway for Trypanosoma Cruzi Growth in the Mammalian Host Cell Cytoplasm," Biochem. Biophys. Res. Commun. 2012, 417, 1002-1006.
DOI: 10.1016/j.bbrc.2011.12.073
S. Kamijo, S. Yokosaka, M. Inoue, "Attachment of Carbonyl Functionalities onto Olefins via Copper-Promoted Radical Reaction of Dichloromethylcyanides," Tetrahedron 2012, 68, 5290-5296.

DOI: 10.1016/j.tet.2012.01.089
D. Urabe, H. Todoroki, K. Masuda, M. Inoue, "Total syntheses of four possible stereoisomers of resolvin E3," Tetrahedron 2012, 68, 3210-3219.

DOI: 10.1016/j.tet.2012.02.045
S. Matsuoka, M. Murai, T. Yamazaki, M. Inoue, "Short polyglutamine peptide forms a high-affinity binding site for thioflavin-T at the N-terminus," Org. Biomol. Chem. 2012, 10, 5787-5790.

DOI: 10.1039/C2OB07157F
Y. Isobe, M. Arita, S. Matsueda, R. Iwamoto, T. Fujihara, H. Nakanishi, R. Taguchi, K. Masuda, K. Sasaki, D. Urabe, M. Inoue, H. Arai, "Identification and structure determination of novel anti-inflammatory mediator resolvin E3, 17,18-dihydroxyeicosapentaenoic acid," J. Biol. Chem. 2012, 287, 10525-10534.
DOI: 10.1074/jbc.M112.340612
S. Matsuoka, J. Mao, and M. Inoue, "Effects of the phosphatidylglycerol head group on the binding of short dermcidin-derived peptides to the phospholipid membrane surface," Tetrahedron Lett. 2012, 53, 1078-1081.

DOI: 10.1016/j.tetlet.2011.12.071

2011

S. Kamijo, T. Hoshikawa, and M. Inoue, "Photochemically Induced Radical Transformation of C(sp³)-H Bonds to C(sp³)-CN Bonds," Org. Lett. 2011, 13, 5928-5931.

DOI: 10.1021/ol202659e
D. Urabe, H. Yamaguchi, M. Inoue, "Application of α-Alkoxy Bridgehead Radical for Coupling of Oxygenated Carbocycles," Org. Lett. 2011, 13, 4778-4781.

DOI: 10.1021/ol201758a
R. Goto, K. Okura, H. Sakazaki, T. Sugawara, S. Matsuoka, M. Inoue, "Synthesis and biological evaluation of triazole analogues of antillatoxin," Tetrahedron 2011, 67, 6659-6672.

DOI: 10.1016/j.tet.2011.05.012
S. Kamijo, Y. Amaoka, M. Inoue, "Direct oxidative installation of nitrooxy group at benzylic positions and its transformation into various functionalities," Tetrahedron Lett. 2011, 52, 4654-4657.

DOI: 10.1016/j.tetlet.2011.06.118
M. Ui, Y. Tanaka, T. Tsumuraya, I. Fujii, M. Inoue, M. Hirama, K. Tsumoto, "Structural and Energetic Hot-spots for the Interaction between a Ladder-like Polycyclic Ether and the Anti-ciguatoxin Antibody 10C9Fab," Mol. BioSyst. 2011, 7, 793-798.

DOI: 10.1039/C0MB00162G
K. Yamaoka, M. Inoue, M. Hirama, "A Study on Mechanisms of Toxic Actions of Ciguatoxins: Existence of Functional Relationship between CTX3C and Charged Residues of Voltage Sensors in Nav1.4 Sodium Channel," Forensic Toxicol. 2011, 29, 125-131.
DOI: 10.1007/s11419-011-0113-6
S. Kamijo, T. Hoshikawa, M. Inoue, "Photoinduced carbamoylation of ethereal C-H bonds using pentafluorophenyl isocyanate," Tetrahedron Lett. 2011, 52, 2885-2888.

DOI: 10.1016/j.tetlet.2011.03.128
S. Matsuoka, N. Shinohara, T. Takahashi, M. Iida, M. Inoue, "Functional Analysis of Synthetic Substructures of Polytheonamide B: A Transmembrane Channel-Forming Peptide," Angew. Chem. Int. Ed. 2011, 50, 4879-4883.

DOI: 10.1002/anie.201101533
S. Yamashita, Y. Ishihara, H. Morita, J. Uchiyama, K. Takeuchi, M. Inoue, M. Hirama, "Stereoselective 6-exo Radical Cyclization Using cis-Vinyl Sulfoxide: Practical Total Synthesis of CTX3C," J. Nat. Prod. 2011, 74, 357-364.

DOI: 10.1021/np100729d
K. Sasaki, D. Urabe, H. Arai, M. Arita, M. Inoue, "Total Synthesis and Bioactivities of Two Proposed Structures of Maresin," Chem. Asian J. 2011, 6, 534-543.

DOI: 10.1002/asia.201000494

2010

S. Kamijo, Y. Amaoka, M. Inoue, "Unified Oxidation Protocol for the Synthesis of Carbonyl Compounds Using a Manganese Catalyst," Synthesis 2010, 2475-2489.

DOI: 10.1055/s-0029-1218809
S. Kamijo, S. Matsumura, M. Inoue, "CCl3CN: A Crucial Promoter of mCPBA-Mediated Direct Ether Oxidation," Org. Lett. 2010, 12, 4195-4197.

DOI: 10.1021/ol1018079
S. Matsuoka, Y. Mizoguchi, H. Itoh, K. Okura, N. Shinohara, M. Inoue, "The effect of sulfur stereochemistry of L-β,β-dimethylmethionine S-oxide on the physicochemical properties of truncated polytheonamides," Tetrahedron Lett. 2010, 51, 4644-4647.

DOI: 10.1016/j.tetlet.2010.06.126
M. Iwatsu, D. Urabe, M. Inoue, "Asymmetric Syntheses of Highly Functionalized Bicyclo[2.2.2]octene Derivatives," Heterocycles 2010, 82, 491-504.

DOI: 10.3987/COM-10-S(E)22
Y. Ishihara, N. Lee, N. Oshiro, S. Matsuoka, S. Yamashita, M. Inoue, M. Hirama, "The first F-ring modified ciguatoxin analogue showing significant toxicity," Chem. Commun. 2010, 46, 2968-2970.

DOI: 10.1039/B924375E
E. O. Balogun, D. K. Inaoka, Y. Kido, T. Shiba, T. Nara, T. Aoki, T. Honma, A. Tanaka, M. Inoue, S. Matsuoka, P. A. M. Michels, S. Harada, K. Kita, "Overproduction, Purification, Crystallization and Preliminary X-ray Diffraction Analysis of Trypanosoma Brucei Gambiense Glycerol Kinase," Acta Crystallogr., Sect. F: Struct. Biol. Cryst. Commun. 2010, F66, 304-308.
DOI: 10.1107/S1744309110000369
Y. Kido, T. Shiba, D. K. Inaoka, K. Sakamoto, T. Nara, T. Aoki, T. Honma, A. Tanaka, M. Inoue, S. Matsuoka, A. Moore, S. Harada, K. Kita, "Crystallization and preliminary crystallographic analysis of cyanide-insensitive alternative oxidase from Trypanosoma brucei brucei," Acta Crystallogr., Sect. F: Struct. Biol. Cryst. Commun. 2010, F66, 275-278.
DOI: 10.1107/S1744309109054062
S. Kamijo, T. Hoshikawa, M. Inoue, "Regio- and Stereoselective Acylation of Saturated Carbocycles via Norrish-Yang Photocyclization," Tetrahedron Lett. 2010, 51, 872-874.

DOI: 10.1016/j.tetlet.2009.12.027
M. Inoue, N. Shinohara, S. Tanabe, T. Takahashi, K. Okura, H. Itoh, Y. Mizoguchi, M. Iida, N. Lee, S. Matsuoka, "Total synthesis of the large non-ribosomal peptide polytheonamide B," Nature Chem. 2010, 2, 280-285.

DOI: 10.1038/nchem.554
K. Okura, S. Matsuoka, R. Goto, M. Inoue, "The Twisted Side Chain of Antillatoxin is Important for Potent Toxicity: Total Synthesis and Biological Evaluation of Antillatoxin and Analogues," Angew. Chem. Int. Ed. 2010, 49, 329-332.

DOI: 10.1002/anie.200905892
S. Kamijo, Y. Amaoka, M. Inoue, "Manganese-Catalyzed Direct Oxidation of Methyl Ethers to Ketones," Chem. Asian J. 2010, 5, 486-489.

DOI: 10.1002/asia.200900420

2009

K. Matoba, T. Nara, T. Aoki, T. Honma, A. Tanaka, M. Inoue, S. Matsuoka, D. K. Inaoka, K. Kita, S. Harada, "Crystallization and Preliminary X-ray Analysis of Aspartate Transcarbamoylase from the Parasitic Protist Trypanosoma Cruzi," Acta Crystallogr., Sect. F: Struct. Biol. Cryst. Commun. 2009, F65, 933.
DOI: 10.1107/S1744309109031959
S. Kasuya, S. Kamijo, M. Inoue, "Direct Construction of 1,3-Diaxial Diol Derivatives by C-H Hydroxylation," Org. Lett. 2009, 11, 3630-3632.

DOI: 10.1021/ol901367m
S. Ogawa, D. Urabe, Y. Yokokura, H. Arai, M. Arita, M. Inoue, "Total Synthesis and Bioactivity of Resolvin E2," Org. Lett. 2009, 11, 3602-2605.

DOI: 10.1021/ol901350g
M. Inoue, N. Lee, T. Tsumuraya, I. Fujii, M. Hirama, "Use of Monoclonal Antibodies as an Effective Strategy for Treatment of Ciguatera Poisoning," Toxicon 2009, 53, 802-805.
DOI: 10.1016/j.toxicon.2009.02.017
K. Yamaoka, M. Inoue, K. Miyazaki, M. Hirama, C. Kondo, E. Kinoshita, H. Miyoshi, I. Seyama, "Synthetic Ciguatoxins Selectively Activate Nav1.8-Derived Chimeric Sodium Channels Expressed in HEK293 Cells," J. Biol. Chem. 2009, 284, 7597-7605.
DOI: 10.1074/jbc.M806481200
K. Hagiwara, M. Himuro, M. Hirama, M. Inoue, "A Concise Route to C2-symmetric Tricyclic Skeleton of Ryanodine," Tetrahedron Lett. 2009, 50, 1035-1037.

DOI: 10.1016/j.tetlet.2008.12.054
N. Lee, M. Inoue, M. Hirama, "Design and Synthesis of a Conformationally Restricted Analogue of the EFGH-Ring System of Ciguatoxin," Heterocycles 2009, 79, 325-330.

DOI: 10.3987/COM-08-S(D)7

2008

M. Inoue, N. Lee, K. Miyazaki, T. Usuki, S. Matsuoka, M. Hirama "Critical Importance of the Nine-Membered F Ring of Ciguatoxin for Potent Bioactivity: Total Synthesis and Biological Evaluation of F-Ring-Modified Analogues," Angew. Chem. Int. Ed. 2008, 47, 8611-8614.
(Selected as Very Important Paper)

DOI: 10.1002/anie.200803921
M. Ui, Y. Tanaka, T. Tsumuraya, I. Fujii, M. Inoue, M. Hirama, K. Tsumoto, "How Protein Recognizes Ladder-like Polycyclic Ethers: Interactions between Ciguatoxin (CTX3C) Fragments and Its specific antibody 10C9," J. Biol. Chem. 2008, 283, 19440-19447.
DOI: 10.1074/jbc.M801282200
K. Nabatame, M. Hirama, M. Inoue, "A Simple Desymmetrization Approach to the Framework of Spiroxins," Heterocycles 2008, 76, 1011-1016.

DOI: 10.3987/COM-08-S(N)70
K. Tsumoto, A. Yokota, Y. Tanaka, M. Ui, T. Tsumuraya, I. Fujii, I. Kumagai, Y. Nagumo, H. Oguri, M. Inoue, M. Hirama, "Critical contribution of aromatic rings to specific recognition of polyether rings.: The case of ciguatoxin CTX3C-ABC and its specific antibody 1C49," J. Biol. Chem. 2008, 283, 12259-12266
DOI: 10.1074/jbc.M710553200
M. Inoue, I. Ohashi, T. Kawaguchi, M. Hirama, "Total Synthesis of the C-1027 Chromophore Core: Extremely Facile Enediyne Formation through SmI2-Mediated 1,2-Elimination," Angew. Chem. Int. Ed. 2008, 47, 1777-1779.

DOI: 10.1002/anie.200704842
K. Iso, M. Inoue, N. Kato, M. Hirama, "Synthesis of the Bicyclo[7.3.0]dodecadiyne Core of the Maduropeptin Chromophore," Chem. Asian J. 2008, 3, 447-453.

DOI: 10.1002/asia.200700310

2007

K. Komano, S. Shimamura, M. Inoue, M. Hirama, "Total Synthesis of the Maduropeptin Chromophore Aglycon," J. Am. Chem. Soc. 2007, 129, 14184-14186.

DOI: 10.1021/ja076671f
M. Inoue, N. Lee, S. Kasuya, T. Sato, M. Hirama, M. Moriyama, Y. Fukuyama, "Total Synthesis and Bioactivity of an Unnatural Enantiomer of Merrilactone A: Development of an Enantioselective Desymmetrization Strategy," J. Org. Chem. 2007, 72, 3065-3075.

DOI: 10.1021/jo0700474
M. Inoue, M. Iwatsu, S. Yamashita, M. Hirama, "A Concise Route to Two Distinct E-Ring Structures of Ciguatoxins," Heterocycles 2007, 72, 327-338.

DOI: 10.3987/COM-06-S(K)16
K. Yoshikawa, M. Inoue, M. Hirama, "Synthesis of the LMN-Ring Fragment of the Caribbean Ciguatoxin C-CTX-1," Tetrahedron Lett. 2007, 48, 2177-2180.

DOI: 10.1016/j.tetlet.2007.01.103
M. Inoue, F. Saito, M. Iwatsu, Y. Ishihara, M. Hirama,　"Convergent Synthesis of the ABCDE-Ring Fragment of the Caribbean Ciguatoxin C-CTX-1," Tetrahedron Lett. 2007, 48, 2171-2175.

DOI: 10.1016/j.tetlet.2007.01.102

2006

M. Inoue, S. Yamashita, Y. Ishihara, M. Hirama, "Two Convergent Routes to the Left Wing Fragment of Ciguatoxin CTX3C Using O,S-Acetals As Key Intermediates," Org. Lett. 2006, 8, 5805-5808.

DOI: 10.1021/ol062350h
M. Inoue, Y. Ishihara, S. Yamashita, M. Hirama, "Convergent Assembly of Polycyclic Ethers via Acyl Radical Addition to Unactivated Enol Ether," Org. Lett. 2006, 8, 5801-5804.

DOI: 10.1021/ol062349i
V. Ghiaroni, H. Fuwa, M. Inoue, M. Sasaki, M. Hirama, T. Yasumoto, G. P. Rossini, G. Scalera,P. Pietra A. Bigiani, "Effect of Ciguatoxin 3C on Voltage-Gated Na+ and K+ Currents in Mouse Taste Cells," Chem. Senses 2006, 31, 673-680.
DOI: 10.1093/chemse/bjl008
T. Tsumuraya, I. Fujii, M. Inoue, A. Tatami, K. Miyazaki, M. Hirama, "Production of monoclonal antibodies for sandwich immunoassay detection of ciguatoxin 51-hydroxyCTX3C," Toxicon 2006, 48, 287-294.
DOI: 10.1016/j.toxicon.2006.05.014
M. Inoue, K. Miyazaki, Y. Ishihara, A. Tatami, Y. Ohnuma, Y. Kawada, K. Komano, S. Yamashita, N. Lee, M. Hirama, "Total Synthesis of Ciguatoxin and 51-HydroxyCTX3C," J. Am. Chem. Soc. 2006, 128, 9352-9354.

DOI: 10.1021/ja063041p
M. Inoue, T. Takahashi, H. Furuyama, M. Hirama, "Structural Factors Governing Stereoselective Heck Reaction for the Construction of the Oxindole Portion of TMC-95A," Synlett 2006, 3037-3040.

DOI: 10.1055/s-2006-951522
M. Inoue, T. Sato, M. Hirama, "Asymmetric Total Synthesis of (-)-Merrilactone A: Use of a Bulky Protective Group as Long-Range Stereocontrolling Element," Angew. Chem. Int. Ed. 2006, 45, 4843-4848.

DOI: 10.1002/anie.200601358
M. Inoue, T. Usuki, N. Lee, M. Hirama, T. Tanaka, F. Hosoi, S. Ohie, T. Otani, "Antitumor Enediyne Chromoprotein C-1027: Mechanistic Investigation of the Chromophore-Mediated Self-Decomposition Pathway," J. Am. Chem. Soc. 2006, 128, 7896-7903.

DOI: 10.1021/ja060724w

2005

T. Usuki, M. Inoue, K. Akiyama, M. Hirama, "ESR Studies on the DNA Cleavage Induced by Enediyne C-1027 Chromophore," Bioorg. & Med. Chem. 2005, 13, 5218-5224.

DOI: 10.1016/j.bmc.2005.05.049

2004

S. Sakamoto, H. Sakazaki, K. Hagiwara, K. Kamada, K. Ishii, T. Noda, M. Inoue, M. Hirama, "A Formal Total Synthesis of (+)-Pinnatoxin A," Angew. Chem. Int. Ed. 2004, 43, 6505-6510.

DOI: 10.1002/anie.200461802
M. Inoue, T. Sasaki, S. Hatano, M. Hirama, "Synthesis of the C-1027 Chromophore Framework through Atropselective Macrolactonization," Angew. Chem. Int. Ed. 2004, 43, 6500-6505.

DOI: 10.1002/anie.200461428
M. Inoue, S. Hatano, M. Kodama, T. Sasaki, T. Kikuchi, M. Hirama, "Synthesis of the Bicyclo[7.3.0]dodecatrienediyne Core of the C-1027 Chromophore," Org. Lett. 2004, 6, 3833-3836.

DOI: 10.1021/ol048494i
M. Inoue, T. Kikuchi, M. Hirama, "Synthesis of the Fully Functionalized Nine-membered Diyne Core of the C-1027 Chromophore," Tetrahedron Lett. 2004, 45, 6439-6442.

DOI: 10.1016/j.tetlet.2004.06.136
T. Usuki, T. Mita, M. J. Lear, P. Das, F. Yoshimura, M. Inoue, M. Hirama, K. Akiyama, S. Tero-Kubota, "Spin-Trapping of 13C-Labeled p-Benzynes, Generated via the Masamune-Bergman Cyclization of Bicyclic Nine-Membered Enediynes," Angew. Chem. Int. Ed. 2004, 43, 5249-5253.

DOI: 10.1002/anie.200454133
M. Inoue, K. Miyazaki, H. Uehara, M. Maruyama, M. Hirama, "First and Second Generation Total Synthesis of Ciguatoxin CTX3C," Proc. Natl. Acad. Sci. U.S.A. 2004, 101, 12013-12018.
DOI: 10.1073/pnas.0401684101
K. Yamaoka, M. Inoue, H. Miyahara, K. Miyazaki, M. Hirama, "A Quantitative and Comparative Study of the Effects of a Synthetic Ciguatoxin CTX3C on the Kinetic Properties of Voltage-dependent Sodium Channels," Br. J. Pharmacol. 2004, 142, 879-889.
DOI: 10.1038/sj.bjp.0705852
M. Inoue, S. Yamashita, A. Tatami, K. Miyazaki, M. Hirama, "A New Stereoselective Synthesis of Ciguatoxin Right Wing Fragments," J. Org. Chem. 2004, 69, 2797-2804.

DOI: 10.1021/jo049877x
M. Inoue, S. Yamashita, M. Hirama, "A New Synthesis of Key Intermediates for the Assembly of Polycyclic Ethers: Yb(OTf)3-promoted Formation of O,S-Acetals from -Fluorosulfides and Alcohols," Tetrahedron Lett. 2004, 45, 2053-2056.

DOI: 10.1016/j.tetlet.2004.01.077
T. Usuki, M. Inoue, M. Hirama, T. Tanaka, "Rational Design of a Supra C-1027: Kinetically Stabilized Analogue of the Antitumor Enediyne Chromoprotein ," J. Am. Chem. Soc. 2004, 126, 3022-3023.

DOI: 10.1021/ja039635z
M. Inoue, H. Zhai, H. Sakazaki, H. Furuyama, Y. Fukuyama, M. Hirama, "TMC-95A, a Reversible Proteasome Inhibitor, Induces Neurite Outgrowth in PC12 Cells," Bioorg. Med. Chem. Lett. 2004, 14, 663-665.

DOI: 10.1016/j.bmcl.2003.11.043

2003

M. Inoue, T. Sato, M. Hirama, "Total Synthesis of Merrilactone A," J. Am. Chem. Soc. 2003, 125, 10772-10773.

DOI: 10.1021/ja036587+
M. Inoue, J. Wang, G.-X. Wang, Y. Ogasawara, M. Hirama, "Divergent Synthesis of the Tetracyclic Ethers of 6-X-7-6 Ring System," Tetrahedron 2003, 59, 5645-5659.

DOI: 10.1016/S0040-4020(03)00913-X
A. Tatami, M. Inoue, H. Uehara, M. Hirama, "A Concise Route to the Right Wing of Ciguatoxin," Tetrahedron Lett. 2003, 44, 5229-5233.

DOI: 10.1016/S0040-4039(03)01214-0
M. Inoue, H. Sakazaki, H. Furuyama, M. Hirama, "Total Synthesis of TMC-95A," Angew. Chem. Int. Ed. 2003, 42, 2654-2657.

DOI: 10.1002/anie.200351130
M. Inoue, M. Hirama, M. Satake, K. Sugiyama, T. Yasumoto, "Inhibition of Brevetoxin Binding to the Voltage-gated Sodium Channel by Gambierol and Gambieric Acid-A," Toxicon 2003, 41, 469-474.
DOI: 10.1016/S0041-0101(02)00369-0
M. Inoue, K. Nabatame, M. Hirama, "A Novel Route to 1,8-Dihydroxynaphthalene-derived Natural Products. Synthesis of (±)-CJ-12,372," Heterocycles 2003, 59, 87-92.

DOI: 10.3987/COM-02-S32

2002

M. Inoue, H. Uehara, M. Maruyama, M. Hirama, "Practical Total Synthesis of Ciguatoxin CTX3C by Improved Protective Group Strategy," Org. Lett. 2002, 4, 4551-4554.

DOI: 10.1021/ol027105m
M. Inoue, G. X. Wang, J. Wang, M. Hirama, "Novel Assembly of Cyclic Ethers by Coupling -Chlorosulfides and Alcohols," Org. Lett. 2002, 4, 3439-3442.

DOI: 10.1021/ol026529d
T. Usuki, M. Inoue, K. Akiyama, M. Hirama, "Spin-trapping Study of DNA Cleavage Induced by Enediyne C-1027 Chromophore," Chem. Lett. 2002, 1148.
DOI: 10.1246/cl.2002.1148
S. Nozaki, Y. Tomioka, T. Hishinuma, M. Inoue, Y. Nagumo, L. R. .Tsuruta, K. Hayashi, T. Matsumoto, Y. Kato, S. Ishiwata, K. Itoh, T. Suzuki, M. Hirama, M. Mizuzaki, "Design, Production, and Characterization of Recombinant Neocarzinostatin Apoprotein in Escherichia coli," J. Biochem. 2002, 131, 729-738.
H. Uehara, T. Oishi, M. Inoue, M. Shoji, Y. Nagumo, M., Kosaka, J.-.Y. Le Brazidec, M. Hirama, "Convergent Synthesis of the HIJKLM Ring Fragment of Ciguatoxin CTX3C," Tetrahedron Symposia-in-Print 2002, 58, 6493-6512.

DOI: 10.1016/S0040-4020(02)00660-9
M. Maruyama, M. Inoue, T. Oishi, H. Oguri, Y. Ogasawara, Y. Shindo, M. Hirama, "Convergent Synthesis of the ABCDE Ring System of Ciguatoxin CTX3C," Tetrahedron Symposia-in-Print 2002, 58, 1835-1851.

DOI: 10.1016/S0040-4020(02)00041-8

2001

M. Hirama, T. Oishi, H. Uehara, M. Inoue, M. Maruyama, H. Oguri, M. Satake, "Total Synthesis of Ciguatoxin CTX3C," Science 2001, 294, 1904-1907.
DOI: 10.1126/science.1065757
M. Inoue, H. Furuyama, H. Sakazaki, M. Hirama, "Stereocontrolled Synthesis of the Nothern Part of Potent Proteasome Inhibitor TMC-95A," Org. Lett. 2001, 3, 2863-2865.

DOI: 10.1021/ol016303v
H. Imai, H. Uehara, M. Inoue, H. Oguri, T. Oishi, M. Hirama, "Convergent Synthesis of the EFGH Ring Fragment of Ciguatoxin CTX3C," Tetrahedron Lett. 2001, 42, 6219-6222.

DOI: 10.1016/S0040-4039(01)01219-9
T. Sasaki, M. Inoue, M. Hirama, "Synthetic Stidies toward C-1027 Chromophore: Construction of a Highly Unsaturated Macrocycle," Tetrahedron Lett. 2001, 42, 5299-5303.

DOI: 10.1016/S0040-4039(01)00959-5
M. Inoue, M. D. Carson, A. J. Frontier, S. J. Danishefsky, "Total Synthesis and Determination of the Absolute Configuration of Frondosin B," J. Am. Chem. Soc. 2001, 123, 1878-1889.

DOI: 10.1021/ja0021060

2000

M. Inoue, A. J. Frontier, S. J. Danishefsky, "The Total Synthesis of Frondosin B," Angew. Chem. Int. Ed. 2000, 39, 761-764.
DOI: 10.1002/(SICI)1521-3773(20000218)39:4<761::AID-ANIE761>3.0.CO;2-I
T. P. P. Petus, M. Inoue, X.-T. Chen, S. J. Danishefsky, "A Fully Synthetic Route to the Neurotrophic Illicinones: Synthesis of Tricycloillicinone and Bicycloillicinone Aldehyde," J. Am. Chem. Soc. 2000, 122, 6160-6168.

DOI: 10.1021/ja000521m
S. Pauillac, M. Sasaki, M. Inoue, J. Naar, P. Branaa, M. Chinain, K. Tachibana, A.-M. Legrand, "Characterization of Mice Antisera Elicited with a Ciguatoxin Tetracyclic Synthetic Ring Fragment (JKLM) Conjugated to Carrier Proteins," Toxicon 2000, 38, 669-685.
DOI: 10.1016/S0041-0101(99)00183-X

1999

M. Inoue, M. Sasaki, K. Tachibana, "A Convergent Synthesis of Decacyclic Ciguatoxin Model Containing the F-M Ring Framework," J. Org. Chem. 1999, 64, 9416-9429.

DOI: 10.1021/jo990989b
M. Sasaki, M. Inoue, K. Takamatsu, K. Tachibana, "Stereocontrolled Synthesis of the JKLM Ring Fragment of Ciguatoxin," J. Org. Chem. 1999, 64, 9399-9415.

DOI: 10.1021/jo990988j
M. Inoue, M. Sasaki, K. Tachibana, "A Convergent Synthesis of the trans-Fused Hexahydrooxonine Ring System and Reproduction of Conformational Behavior Shown by Ring F of Ciguatoxin," Tetrahedron 1999, 55, 10949-10970.

DOI: 10.1016/S0040-4020(99)00620-1

1998

M. Sasaki, H. Fuwa, M. Inoue, K. Tachibana, "New Strategy for Convergent Synthesis of trans-Fused Polyether Frameworks Based on Palladium-Catalyzed Suzuki Cross-Coupling Reaction," Tetrahedron Lett. 1998, 39, 9027-9030.

DOI: 10.1016/S0040-4039(98)02025-5
M. Sasaki, M. Inoue, T. Noguchi, A. Takeichi, K. Tachibana, "Convergent and Stereoselective Method for Synthesis of O-Linked Oxepane Ring System by Intramolecular Radical Cyclization," Tetrahedron Lett. 1998, 39, 2783-2786.

DOI: 10.1016/S0040-4039(98)00338-4
M. Inoue, M. Sasaki, K. Tachibana, "Synthetic Studies on Ciguatoxin: A Convergent Strategy for Construction of the F-M Ring Framework," Angew. Chem. Int. Ed. 1998, 37, 965-969.
DOI: 10.1002/(SlCl)1521-3773(19980420)37:7<965::AID-ANIE965>3.0.CO;2-P

1997

M. Inoue, M. Sasaki, K. Tachibana, "Construction of Fused Oxonene Ring and Reproduction of Conformational Behavior Shown by Ring F of Ciguatoxin," Tetrahedron Lett. 1997, 38, 1611-1614.

DOI: 10.1016/S0040-4039(97)00125-1

1994

M. Sasaki, M. Inoue, K. Tachibana, "Synthetic Studies toward Ciguatoxin. Stereocontrolled Construction of the KLM Ring Fragment," J. Org. Chem. 1994, 59, 715-717.
DOI: 10.1021/jo00083a008

Reviews and Accounts

Y. Hikone, M. Nagatomo, M. Inoue, "Development of Streamlined Processes for Construction of Complex Natural Products: Three Synthesis of Resiniferatoxin," J. Synth. Org. Chem., Jpn. 2023, 81, 1136-1149.

DOI: 10.5059/yukigoseikyokaishi.81.1136
H. Itoh, M. Inoue, "Development of a High-Throughput Strategy for Functional Enhancement and Alteration of Antibacterial Natural Products," J. Synth. Org. Chem., Jpn. 2021, 79, 996-1004.

DOI: 10.5059/yukigoseikyokaishi.79.996
H. Fujino, M. Nagatomo, M. Inoue, "Total Syntheses of Hikosamine and Hikizimycin," J. Org. Chem. 2021, 86, 16220–16230.
(Selected as the cover picture link)

DOI: 10.1021/acs.joc.1c01773
T. Shimakawa, K. Hagiwara, M. Inoue, "Total Synthesis of Talatisamine: Exploration of Convergent Synthetic Strategies," Bull. Chem. Soc. Jpn. 2021, 94, 973-983.

DOI: 10.1246/bcsj.20200400
M. Nagatomo, M. Inoue, "Convergent Assembly of Highly Oxygenated Natural Products Enabled by Intermolecular Radical Reactions," Acc. Chem. Res. 2021, 54, 595-604.

DOI: 10.1021/acs.accounts.0c00792
H. Itoh, M. Inoue, "Full solid-phase total synthesis of macrocyclic natural peptides using four-dimensionally orthogonal protective groups," Org. Biomol. Chem. 2019, 17, 6519-6527.

DOI: 10.1039/C9OB01130G
D. Urabe, M. Inoue, "Convergent Total Synthesis of Bioactive Cardenolides" J. Synth. Org. Chem., Jpn 2019, 77, 452-461.
DOI: 10.5059/yukigoseikyokaishi.77.452
H. Itoh, M. Inoue, "Comprehensive Structure–Activity Relationship Studies of Macrocyclic Natural Products Enabled by Their Total Syntheses," Chem. Rev. 2019, 119, 10002-10031.

DOI: 10.1021/acs.chemrev.9b00063
M. Inoue, "Evolution of Radical-Based Convergent Strategies for Total Syntheses of Densely Oxygenated Natural Products," Acc. Chem. Res. 2017, 50, 460-464.

DOI: 10.1021/acs.accounts.6b00475
T. Asaba, D. Urabe, M. Inoue, "Asymmetric Total Synthesis of Crotophorbolone: Construction of the 5/7/6-Fused Ring System via an α-Alkoxy Bridgehead Radical Reaction," Bull. Chem. Soc. Jpn. 2016, 89, 1137-1144.

DOI: 10.1246/bcsj.20160208
D. Urabe, H. Todoroki, M. Inoue, "Asymmetric Total Synthesis of (－)-4-Hydroxyzinowol, a Highly Oxygenated Dihydro-β-Agarofuran," J. Synth. Org. Chem., Jpn 2015, 73, 1081-1091.
DOI: 10.5059/yukigoseikyokaishi.73.1081
D. Urabe, T. Asaba, M. Inoue, "Convergent Strategies in Total Syntheses of Complex Terpenoids," Chem. Rev. 2015, 115, 9207-9231.

DOI: 10.1021/cr500716f
M. Inoue, "Chemical Construction and Structural Permutation of Neurotoxic Natural Product, Antillatoxin: Importance of the Three-Dimensional Structure of the Bulky Side Chain," Proc. Jpn. Acad., Ser. B 2014, 90, 56-66.
DOI: 10.2183/pjab.90.56
T. Kuranaga, Y. Sesoko, M. Inoue, "Cu-mediated enamide formation in the total synthesis of complex peptide natural products," Nat. Prod. Rep. 2014, 31, 514-532.

DOI: 10.1039/C3NP70103D
H. Itoh, M. Inoue, "Chemical Construction and Structural Permutation of Potent Cytotoxin Polytheonamide B: Discovery of Artificial Peptides with Distinct Functions," Acc. Chem. Res. 2013, 46, 1567-1578.

DOI: 10.1021/ar300315p
M. Inoue, "Total synthesis and functional analysis of non-ribosomal peptides," Chem. Rec. 2011, 11, 284-294.

DOI: 10.1002/tcr.201100014
M. Inoue, S. Matsuoka, "Convergent Total Synthesis of the Complex Non-Ribosomal Peptide Polytheonamide B," Isr. J. Chem. 2011, 51, 346-358.
DOI: 10.1002/ijch.201100002
S. Matsuoka, M. Inoue, "Application of REDOR NMR in Natural Product Chemistry," Chem. Commun. 2009, 5664-5675.
DOI: 10.1039/B910230B
D. Urabe, M. Inoue, "Total Syntheses of Sesquiterpenes from Illicium Species," Tetrahedron 2009, 65, 6271-6289.

DOI: 10.1016/j.tet.2009.06.010
M. Inoue, T. Saito, M. Hirama "Total Synthesis of Merrilactone A: Long-Range Stereocontrol and Asymmetric Desymmetrization" J. Synth. Org. Chem., Jpn 2007, 65, 419-429.
DOI: 10.5059/yukigoseikyokaishi.65.419
M. Inoue, "Exploring the Chemistry and Biology of Antitumor Enediyne Chromoprotein C-1027," Bull. Chem. Soc. Jpn. 2006, 79, 501-510.
DOI: 10.1246/bcsj.79.501
M. Inoue, "Convergent Strategies for Syntheses of trans-Fused Polycyclic Ethers," Chem. Rev. 2005, 105, 4379-4405.

DOI: 10.1021/cr0406108
M. Inoue, M. Hirama, "Evolution of a Practical Total Synthesis of Ciguatoxin CTX3C," Acc. Chem. Res. 2004, 37, 961-968.

DOI: 10.1021/ar0301577
M. Inoue, "Convergent Syntheses of Polycyclic Ethers. Illustrations of the Utility of Acetal-linked Intermediates," Org. Biomol. Chem. 2004, 2, 1811-1817.

DOI: 10.1039/B407187E
M. Inoue, M. Hirama, "Total Synthesis of Ciguatoxin CTX3C, a Causative Toxin of Ciguatera Seafood Poisoning," Synlett 2004, 577-595.

DOI: 10.1055/s-2004-817767
M. Sasaki, M. Inoue "Synthetic Studies on Polyether Natural Products: New Synthetic Methods for Construction of Medium-Sized Cyclic Ethers and Convergent Coupling of Polyether Fragments," J. Synth. Org. Chem., Jpn 2001, 59, 193-205.
DOI: 10.5059/yukigoseikyokaishi.59.193

Book Chapters

伊藤寛晃, 井上将行, "ペプチド系複雑天然物の全合成とその応用展開," 実験医学増刊 Vol. 43 No.2 中分子ペプチド医薬, 編集　菅裕明, 羊土社, pp 226-231 (2025).
H. Fujino, M. Inoue, "Convergent Total Synthesis of Hikizimycin: Development of New Radical-Based and Protective Group Strategies," In Modern Natural Product Synthesis, M. Nakada, K. Tanino, K. Nagasawa, S. Yokoshima, Ed.; Springer: Singapore, 2024; pp 127-144.
DOI: 10.1007/978-981-97-1619-7_6
H. Fujino, M. Inoue, "Fragmentation Reactions," Reference Module in Chemistry, Molecular Sciences and Chemical Engineering 2023
DOI: 10.1016/B978-0-323-96025-0.00010-7
井上将行 "巨大複雑天然物の全合成経路を構築するー合成終盤でのデッドエンドを回避した二つの方策," ドラマチック有機合成化学　感動の瞬間 100, 編集　有機合成化学協会，東京化学同人, pp 106-107 (2023).
Submitted by H. Huang, Z. Xu, G.-J. Deng, Checked by H. Morozumi, K. Hagiwara, M. Inoue, "Synthesis of 2-Phenyl-4,6-bis(trifluoromethyl)pyridine via NH4I/Na2S2O4-Mediated Cyclization of Ketoxime Acetates," Org. Synth. 2023, 100, 248-270.
DOI: 10.15227/orgsyn.100.0248
Submitted by Y. Xue, A. Parsad, G. Dong, Checked by J. Han, M. Nagatomo, M. Inoue, "α-Arylation of Cyclopentanones by Palladium/Enamine Cooperative Catalysis," Org. Synth. 2023, 100, 99-112.
DOI: 10.15227/orgsyn.100.0099
井上将行 "全合成戦略と天然物機能のアップグレード," 有機化学イノベーション（現代化学増刊４７）, 監修　山本尚，東京化学同人, pp 209-223 (2023).
Submitted by D. P. Graeff, N. J. Sims, Q. R. Savage, R. K. Jackson, III, A. C. Jackson, D. M. Lawson, M. R. Wixom, J. L. Wood, Checked by Y. Shiga, H. Fujino, M. Inoue, "Preparation of N-Boc-3-methylpyrrole via Anionic Rearrangement," Org. Synth. 2023, 100, 61-83.
DOI: 10.15227/orgsyn.100.0061
Submitted by M. Varghese, H. E. Caputo, R. Xiao, A. Balijepalli, A. Hamoud, M. W. Grinstaff, Checked by K. Oga, M. Nagatomo, M. Inoue, "Stereoselective [2+2] Cycloadditions: Synthesis of a Tri-O-Bn-D-Glucal-derived β-Lactam," Org. Synth. 2021, 98, 491-508.
DOI: 10.15227/orgsyn.098.0491
Submitted by J. S. Kingsbury, V. L. Rendina, J. S. Burman, B. A. Smolarski, Checked by J. Taguchi, H. Fujino, M. Inoue, "Catalytic Diazoalkane-Carbonyl Homologation: Synthesis of 2,2-Diphenylcycloheptanone and Other Quaternary or Tertiary Arylalkanones and Spirocycles by Ring Expansion," Org. Synth. 2021, 98, 343-362.
DOI: 10.15227/orgsyn.098.0343
Submitted by A. K. Bodnar, A. Turlik, D. Huang, W. Butcher, J. K. Lew, T. R. Newhouse, Checked by A. Takeuchi, H. Itoh, M. Inoue, "Preparation of Hindered Aniline CyanH and Application in the Allyl-Ni-Catalyzed α,β-Dehydrogenation of Carbonyls," Org. Synth. 2021, 98, 263-288.
DOI: 10.15227/orgsyn.098.0263
Submitted by M. Krzeszewski, M. Tasior, M. Grzybowski, D. T. Gryko, Checked by S. Nakamura, K. Hagiwara, M. Inoue, "Synthesis of Tetraaryl-, Pentaaryl-, and Hexaaryl-1,4-dihydropyrrolo[3,2-b]pyrroles," Org. Synth. 2021, 98, 242-262.
DOI: 10.15227/orgsyn.098.0242
Submitted by N. Zhu, W.-M. Wan, H. Bao, Checked by Y. Watanabe, K. Hagiwara, M. Inoue, "Reductive Deuteration of Ketones with Magnesium and D2O for the Synthesis of α-Deutero-o-methyl-benzhydrol," Org. Synth. 2021, 98, 51-67.
DOI: 10.15227/orgsyn.098.0051
Submitted by Y. Chen, Q. Chen, L. Tan, L. Chen, X. Wang, Checked by Y. Komori, M. Nagatomo, M. Inoue, "Preparation of 1H-Indazole-3-carbonitrile," Org. Synth. 2020, 97, 314-326.
DOI: 10.15227/orgsyn.097.0314
Submitted by J. R. Lizza, P. Wipf, Checked by K. Miura, H. Itoh, M. Inoue, "Synthesis of 4-Nitrophenyl (2,2,6,6-Tetramethylpiperidin-1-yl) Carbonate (NPTC) for N-Protection of L-Phenylalanine Ethyl Ester," Org. Synth. 2020, 97, 96-124.
DOI: 10.15227/orgsyn.097.0096
Submitted by J. Klepp, W. Dillon, Y. Lin, P. Feng, B. W. Greatrex, Checked by Y. Imamura, M. Nagatomo, M. Inoue, "Preparation of (-)-Levoglucosenone from Cellulose Using Sulfuric Acid in Polyethylene Glycol," Org. Synth. 2020, 97, 38-53.
DOI: 10.15227/orgsyn.097.0038
Submitted by S. M. Engle, T. R. Kirkner, C. B. Kelly, Checked by S. Shimizu, K. Hagiwara, M. Inoue, "Preparation of 2,4,5,6-Tetra(9H-carbazol-9-yl)isophthalonitrile," Org. Synth. 2019, 96, 455-473.
DOI: 10.15227/orgsyn.096.0455
Submitted by B. J. Simmons, M. Ramirez, N. K. Garg, Checked by T. Shimakawa, K. Hagiwara, M. Inoue, "Facile Reduction of Amides Using Nickel Catalysis: Reduction of 12-Aminododecanolactam," Org. Synth. 2019, 96, 436-454.
DOI: 10.15227/orgsyn.096.0436
Submitted by Y. Kawashima, T. Furukawa, N. Chatani, M. Tobisu, Checked by T. Fukuda, M. Nagatomo, M. Inoue, “Nickel-Catalyzed Cross-Coupling of 2-Methoxynaphthalene with Methyl 4-(5,5-dimethyl-1,3,2-dioxaborinan-2-yl)benzoate,” Org. Synth. 2019, 96, 36-52.
DOI: 10.15227/orgsyn.096.0036
長友優典, 井上将行, “リアノダンジテルペンの統一的全合成,”　天然有機化合物の全合成　独創的なものづくりの反応と戦略(CSJカレントレビュー 27) (日本化学会　編), 化学同人, pp 103-109 (2018).
井上将行, 占部大介, “全合成の現在と未来：戦略面から見た全合成と人工分子創製の重要性,”　天然有機化合物の全合成　独創的なものづくりの反応と戦略(CSJカレントレビュー 27) (日本化学会　編), 化学同人, pp 20-23 (2018).
井上将行, “失敗をオリジナリティーにつなげる戦略,”　東大エグゼクティブ・マネジメント　デザインする思考力 (東大EMP 横山禎徳　編), 東京大学出版, pp 205-242 (2014).
M. Inoue, D. Urabe, "Symmetry-Driven Total Synthesis of Merrilactone A and Resolvin E2," Strategy and Tactics in Organic Synthesis 2013, 9, pp 149-175.
井上将行, ブラウン有機化学, 東京化学同人, (2014).
上條真,　井上将行, "Wacker酸化," トップドラッグから学ぶ創薬化学, 東京化学同人, pp 168-168 (2012).
占部大介, 井上将行, "オレフィンメタセシス," トップドラッグから学ぶ創薬化学, 東京化学同人, pp 128-129 (2012).
石山備凡, 井上将行, "Michael反応," トップドラッグから学ぶ創薬化学, 東京化学同人, pp 121-121 (2012).
井上将行, “革新的戦略による天然物全合成,” 化学のブレークスルー, 化学同人, pp 30-34 (2011).
井上将行, 佐藤隆章, “[2+2]光付加環化反応,” 天然物合成で活躍した反応: 実験のコツとポイント, 化学同人, pp 62-63 (2011).
井上将行 "対称性を利用したメリラクトンAの全合成―遠隔不斉誘導と不斉非対称化―," 創薬科学の魅力－東京大学大学院薬学系研究科からの発信, 廣川書店, pp 105-117 (2010).
井上将行，佐藤隆章，平間正博 "対称性を利用したメリラクトンAの全合成―遠隔不斉誘導と不斉非対称化―," 天然物全合成の最新動向, 監修　北泰行，シーエムシー出版, pp 3-17 (2009).
井上将行, "革新的戦略による天然物全合成," 別冊化学『化学のブレークスルー【有機化学編】』, 化学同人, pp 22-27 (2009).
平間正博, 井上将行, "シガトキシン," 大学院講義　有機化学　改訂第2版, 編集代表　野依良治, 東京化学同人, II巻 6·8, (2015).
M. Inoue, S. Yamashita, "Product Class: 5-, 6- and Larger Ring Oxacycloalkanes," Science of Synthesis, ed. by C. J. Forsyth, Thieme, Chapter 37.5.
S. J. Danishefsky, M. Inoue, D. Trauner, "Synthesis of Immunomodulatory Marine Natural Products," The Role of Natural Products in Drug Discovery, eds. by J. Mulzer, R. Bohlmann, Springer-Verlag, 2000, pp. 1-24.

Others

M. Inoue, L. R. Malins, H. Renata, "Radical Reactions for the Construction and Transformation of Complex Molecules," Org. Lett. 2024, 26 (37), 7775-7777.
DOI: 10.1021/acs.orglett.4c03159
長友優典, 今村祐亮, 井上将行, "抗がん剤タキソールの全合成――ラジカル反応を活用した新しい合成戦略とその展開," 化学 2023, 78 (7), 33-37.
Link
Masayuki Inoue, Kotaro Tokumoto, Takuya Kaji, Hiroaki Itoh, "Design, Construction, and Screening of a One-Bead-One-Compound Library for Discovery of Potent Analogues of Antibiotic Lysocin E," MEDCHEM NEWS 2020, 30 (2), 84-88.
DOI: 10.14894/medchem.30.2_84
M. Inoue, D. Trauner, "In Honor of Professor Samuel J. Danishefsky," J. Antibiot. 2019, 72, 324.
DOI: 10.1038/s41429-019-0182-z
井上将行, "新・化学を創ってゆく人びと：井上将行教授に聞く," 化学 2018, 73 (10), 12-18.
井上将行, 長友優典, 占部大介, "ラジカル反応を基盤とした高酸化度天然物の収束的合成戦略," ファルマシア 2017, 53, 860-864.
長友優典, 井上将行, "リアノジン類の統一的全合成-多様性を志向した共通中間体の設計戦略," 化学 2016, 71 (4), 47-48.
(Associated Link: Link1)
伊藤寛晃, 井上将行, "脂質を見分ける天然物," 化学 2015, 70 (8), 64-65.
M. Inoue, "A Special Issue on Total Synthesis," Chem. Rec. 2014, 14, 579.
T. Hoshikawa, M. Nagatomo, M. Inoue, “Pentafluorophenyl Isocyanate,” e-EROS 2013, RN01621.
DOI: 10.1002/047084289X.rn01621
S. Kamijo, M. Inoue, "4,4',4"-tri-tert-butyl-2,2':6',2"-terpyridine," e-EROS 2012, RN01474.
DOI: 10.1002/047084289X.rn01474
M. Inoue, "Author Profile," Angew. Chem. Int. Ed. 2011, 50, 9016.
DOI: 10.1002/anie.201103732
井上将行, 占部大介, "ラジカル反応を基軸とする複雑天然物の合成," 化学工業 2011, 62, 594-596.
井上将行, 松岡茂, "イオンチャネルを形成する巨大ペプチド系天然物の全合成," ペプチドニュースレター 2010, 78, 1-3.
井上将行, "巨大天然物の全合成と機能," 化学と工業 2009, 62, 138-141.
井上将行, 平間正博, "高反応性エンジイン系抗腫瘍性物質の機能と合成," ファルマシア 2008, 44, 130-134.
M. Inoue, "Nature Journal Club," Nature 2008, 452, 257.
DOI: 10.1038/452257a
M. Inoue, "Zippier synthesis in water," Nature 2007, 449, 667-669.
DOI: 10.1038/449667a
M. Inoue, K. Suzuki, "Receiving the 1st Merck Banyu Lectureship Award (MBLA)," J. Synth. Org. Chem., Jpn 2006, 64, 263-268.
DOI: 10.5059/yukigoseikyokaishi.64.263
井上将行, "抗生物質をアップグレードする," 化学 2005, 60 (9), 68-69.
井上将行, "２０年後の有機合成はどこへ行くのか," 創立60周年記念ポスト事業『有機合成化学と精密化学工業の将来一若手研究者は語る一』第4回有機合成化学協会東北北海道支部, 東北地区からの報告有機合成化学協会誌 2004, 62, 836-837.
DOI: 10.5059/yukigoseikyokaishi.62.833
井上将行, "留学のすすめ," 化学 2002, 57 (9), 22-23.
井上将行, "生理活性発現機構解明を目的とした天然物の全合成研究," 化学 2002, 57 (2), 31-32.

Hiroaki Itoh

Original Papers

2024

Y. Lin, H. Itoh, S. Dan, M. Inoue, "Methyl scanning approach for enhancing the biological activity of the linear peptidic natural product, efrapeptin C," Chem. Sci. 2024, 15, 19390-19399.

DOI: 10.1039/D4SC04384G

2023

J. Fu, Y. Nakata, H. Itoh, S. Panthee, H. Hamamoto, K. Sekimizu, M. Inoue, "Molecular Editing Enhances Oxidation Resistance of Menaquinone-Targeting Antibiotics Lysocin E and WAP-8294A2," Chem. Eur. J. 2023, 29, e202301224.
DOI: 10.1002/chem.202301224
Y. Nakata, J. Fu, H. Itoh, S. Panthee, H. Hamamoto, K. Sekimizu, M. Inoue, "Construction of Five Tryptophan Isomers and Application of the Isomers to Solid-Phase Total Syntheses of Lysocin E Derivatives," Chem. Eur. J. 2023, 29, e202301225.
DOI: 10.1002/chem.202301225
Y.-W. Xue, K. Miura, H. Itoh, M. Inoue, "C-Terminal Modification of Polytheonamide B Uncouples Its Dual Functions in MCF-7 Cancer Cells," Chem. Commun. 2023, 59, 3914-3917.

DOI: 10.1039/D2CC05915K

2022

Y.-W. Xue, H. Itoh, S. Dan, M. Inoue, "Gramicidin A Accumulates in Mitochondria, Reduces ATP Levels, Induces Mitophagy, and Inhibits Cancer Cell Growth," Chem. Sci. 2022, 13, 7482-7491.

DOI: 10.1039/D2SC02024F

2021

H. Hamamoto, S. Panthee, A. Paudel, K. Ishii, J. Yasukawa, J. Su, A. Miyashita, H. Itoh, K. Tokumoto, M. Inoue, K. Sekimizu, "Serum apolipoprotein A-I potentiates the therapeutic efficacy of lysocin E against Staphylococcus aureus," Nat. Commun. 2021, 12, 6364.
DOI: 10.1038/s41467-021-26702-0
A. Takeuchi, H. Itoh, M. Inoue, "¹⁸O/¹⁶O-Encoding Strategy for Microscale Stereochemical Determination of Peptidic Natural Products," Chem. Asian J. 2021, 16, 2447-2452.

DOI: 10.1002/asia.202100674
K. Kamiya, H. Itoh, M. Inoue, "Generation and Biological Evaluation of Degraded Derivatives of the Three E/Z-Isomers of Yaku'amide B," J. Nat. Prod. 2021, 84, 1854–1859.

DOI: 10.1021/acs.jnatprod.1c00339
K. Kamiya, K. Miura, H. Itoh, M. Inoue, "Divergent Solid‐Phase Synthesis and Biological Evaluation of Yaku’amide B and Its Seven E/Z Isomers," Chem. Eur. J. 2021, 27, 1088-1093.
(Selected as Hot Paper)

DOI: 10.1002/chem.202003858

2020

S. Shimizu, K. Hagiwara, H. Itoh, M. Inoue, "Unified Total Synthesis of Five Bufadienolides," Org. Lett. 2020, 22, 8652-8657.
(Selected as Most Read Articles of the month)

DOI: 10.1021/acs.orglett.0c03251
Y. Iwahashi, Y. Toyama, S. Imai, H. Itoh, M. Osawa, M. Inoue, I. Shimada, "Conformational equilibrium shift underlies altered K⁺ channel gating as revealed by NMR," Nat. Commun. 2020, 11, 5168.
DOI: 10.1038/s41467-020-19005-3
Y. Takada, H. Itoh, A. Paudel, S. Panthee, H. Hamamoto, K. Sekimizu, M. Inoue, "Discovery of gramicidin A analogues with altered activities by multidimensional screening of a one-bead-one-compound library," Nat. Commun. 2020, 11, 4935.
(Highlighted in press releases of UTokyo FOCUS, link)
(Selected as Nature Communications Editors' Highlights, link)

DOI: 10.1038/s41467-020-18711-2
J. Mao, H. Itoh, K. Sakurai, M. Inoue, "Phospholipid-Dependent Functions of a Macrocyclic Analogue of the Ion-Channel-Forming Antibiotic Gramicidin A," Chem. Pharm. Bull. 2020, 68, 173-178.

DOI: 10.1248/cpb.c19-00967
H. Itoh, K. Miura, K. Kamiya, T. Yamashita, M. Inoue, "Solid‐Phase Total Synthesis of Yaku’amide B Enabled by Traceless Staudinger Ligation," Angew. Chem. Int. Ed. 2020, 59, 4564-4571.

DOI: 10.1002/anie.201916517

2019

Y.-W. Xue, A. Hayata, H. Itoh, M. Inoue, "Biological Effects of a Simplified Synthetic Analogue of Ion‐Channel‐Forming Polytheonamide B on Plasma Membrane and Lysosomes," Chem. Eur. J. 2019, 25, 15198-15204.
(Selected as Hot Paper)

DOI: 10.1002/chem.201903974
H. Itoh, K. Tokumoto, T. Kaji, A. Paudel, S. Panthee, H. Hamamoto, K. Sekimizu, M. Inoue, "Development of a high-throughput strategy for discovery of potent analogues of antibiotic lysocin E," Nat. Commun. 2019, 10, 2992.
(Highlighted in press releases of UTokyo FOCUS, link)
(Selected as Nature Communications Editor's Highlights. link)

DOI: 10.1038/s41467-019-10754-4

2018

D. Urabe, Y. Nakagawa, K. Mukai, K. Fukushima, N. Aoki, H. Itoh, M. Nagatomo, M. Inoue, "Total synthesis and biological evaluation of 19-hydroxysarmentogenin-3-O-a-L-rhamnoside, trewianin, and their aglycons," J. Org. Chem. 2018, 83, 13888-13910.

DOI: 10.1021/acs.joc.8b02219
K. Kitamura, H. Itoh, K. Sakurai, S. Dan, M. Inoue, "Target Identification of Yaku’amide B and Its Two Distinct Activities against Mitochondrial FoF1-ATP Synthase," J. Am. Chem. Soc. 2018, 140, 12189-12199.
(Selected as Spotlights on Recent JACS Publications)

DOI: 10.1021/jacs.8b07339
A. Hayata, H. Itoh, M. Inoue, "Solid-Phase Total Synthesis and Dual Mechanism of Action of the Channel-Forming 48-mer Peptide Polytheonamide B," J. Am. Chem. Soc. 2018, 140, 10602-10611.

DOI: 10.1021/jacs.8b06755
Y. Kofuku, T. Yokomizo, S. Imai, Y. Shiraishi, M. Natsume, H. Itoh, M. Inoue, K. Nakata, S. Igarashi, H. Yamaguchi, T. Mizukoshi, E. Suzuki, T. Ueda, I. Shimada, "Deuteration and selective labeling of alanine methyl groups of β₂-adrenergic receptor expressed in a baculovirus-insect cell expression system," J. Biomol. NMR 2018, 71, 185-192.
DOI: 10.1007/s10858-018-0174-5
H. Itoh, K. Tokumoto, T. Kaji, A. Paudel, S. Panthee, H. Hamamoto, K. Sekimizu, M. Inoue, "Total Synthesis and Biological Mode of Action of WAP-8294A2: A Menaquinone-Targeting Antibiotic," J. Org. Chem. 2018, 83, 6924-6935.
(Selected as ACS editors' choice)
(The Journal of Organic Chemistry Outstanding Publication of the Year Lectureship Award)
(Selected as the three most read papers in JOC in 2018)

DOI:10.1021/acs.joc.7b02318

2016

T. Kaji, M. Murai, H. Itoh, J. Yasukawa, H. Hamamoto, K. Sekimizu, M. Inoue, "Total Synthesis and Functional Evaluation of Fourteen Derivatives of Lysocin E: Importance of Cationic, Hydrophobic, and Aromatic Moieties for Antibacterial Activity," Chem. Eur. J. 2016, 22, 16912-16919.

DOI:10.1002/chem.201604022
H. Mutoh, Y. Sesoko, T. Kuranaga, H. Itoh, M. Inoue, "Total Synthesis and Functional Evaluation of Fourteen Stereoisomers of Yaku’amide B. Importance of Stereochemistry for Hydrophobicity and Cytotoxicity," Org. Biomol. Chem. 2016, 14, 4199-4204.
(Selected as Hot Article)
(Selected as 2016's Most Popular Article)

DOI: 10.1039/C6OB00640J
A. Hayata, H. Itoh, S. Matsutaka, M. Inoue, "Dual Chemical Modification of a Polytheonamide Mimic: Rational Design and Synthesis of Ion-Channel-Forming 48-mer Peptides with Potent Cytotoxicity," Chem. Eur. J. 2016, 22, 3370-3377.
(Selected as Very Important Paper)

DOI: 10.1002/chem.201504632

2014

H. Itoh, S. Matsutaka, T. Kuranaga, M. Inoue, "Control of the cytotoxicity of dansylated polytheonamide mimic, an artificial peptide ion channel, by modification of the N-terminal structure," Tetrahedron Lett. 2014, 55, 728-731.

DOI: 10.1016/j.tetlet.2013.12.007
H. Itoh, M. Inoue, "Antibody-mediated functional control of a dansylated polytheonamide mimic," Chem. Commun. 2014, 50, 939-941.

DOI: 10.1039/C3CC48348G

2013

H. Itoh, M. Inoue, "Structural Permutation of Potent Cytotoxin, Polytheonamide B: Discovery of Cytotoxic Peptide with Altered Activity," ACS Med. Chem. Lett. 2013, 4, 52-56.

DOI: 10.1021/ml300264c

2012

H. Itoh, S. Matsuoka, M. Kreir, M. Inoue, "Design, Synthesis and Functional Analysis of Dansylated Polytheonamide Mimic: An Artificial Peptide Ion Channel," J. Am. Chem. Soc. 2012, 134, 14011-14018.

DOI: 10.1021/ja303831a
N. Shinohara, H. Itoh, S. Matsuoka, M. Inoue, "Selective Modification of the N-Terminal Structure of Polytheonamide B Significantly Changes its Cytotoxicity and Activity as an Ion Channel," ChemMedChem 2012, 7, 1770-1773.

DOI: 10.1002/cmdc.201200142

2010

S. Matsuoka, Y. Mizoguchi, H. Itoh, K. Okura, N. Shinohara, M. Inoue, "The effect of sulfur stereochemistry of L-β,β-dimethylmethionine S-oxide on the physicochemical properties of truncated polytheonamides," Tetrahedron Lett. 2010, 51, 4644-4647.

DOI: 10.1016/j.tetlet.2010.06.126
M. Inoue, N. Shinohara, S. Tanabe, T. Takahashi, K. Okura, H. Itoh, Y. Mizoguchi, M. Iida, N. Lee, S. Matsuoka, "Total synthesis of the large non-ribosomal peptide polytheonamide B," Nature Chem. 2010, 2, 280-285.

DOI: 10.1038/nchem.554

Reviews and Accounts

H. Itoh, "Total Synthesis and Functional Analysis of Complex Peptidic Natural Products and Their Artificial Analogues," YAKUGAKU ZASSHI 2022, 142, 561-571.
DOI: 10.1248/yakushi.22-00042
H. Itoh, M. Inoue, "Development of a High-Throughput Strategy for Functional Enhancement and Alteration of Antibacterial Natural Products," J. Synth. Org. Chem., Jpn. 2021, 79, 996-1004.

DOI: 10.5059/yukigoseikyokaishi.79.996
H. Itoh, M. Inoue, "Full solid-phase total synthesis of macrocyclic natural peptides using four-dimensionally orthogonal protective groups," Org. Biomol. Chem. 2019, 17, 6519-6527.

DOI: 10.1039/C9OB01130G
H. Itoh, M. Inoue, "Comprehensive Structure–Activity Relationship Studies of Macrocyclic Natural Products Enabled by Their Total Syntheses," Chem. Rev. 2019, 119, 10002-10031.

DOI: 10.1021/acs.chemrev.9b00063
H. Itoh, M. Inoue, "Chemical Construction and Structural Permutation of Potent Cytotoxin Polytheonamide B: Discovery of Artificial Peptides with Distinct Functions," Acc. Chem. Res. 2013, 46, 1567-1578.

DOI: 10.1021/ar300315p

Book Chapters

伊藤寛晃, 井上将行, "ペプチド系複雑天然物の全合成とその応用展開," 実験医学増刊 Vol. 43 No.2 中分子ペプチド医薬, 編集　菅裕明, 羊土社, pp 226-231 (2025).
H. Itoh, “Discovery of Natural Product Analogues with Altered Activities by a High-Throughput Strategy,”　 New Tide of Natural Product Chemistry, Springer, Singapore, pp 333-354 (2023).
DOI: 10.1007/978-981-99-1714-3_16
Submitted by A. K. Bodnar, A. Turlik, D. Huang, W. Butcher, J. K. Lew, and T. R. Newhouse, Checked by A. Takeuchi, H. Itoh, M. Inoue, "Preparation of Hindered Aniline CyanH and Application in the Allyl-Ni-Catalyzed α,β-Dehydrogenation of Carbonyls," Org. Synth. 2021, 98, 263-288.
DOI: 10.15227/orgsyn.098.0263
Submitted by J. R. Lizza, P. Wipf, Checked by K. Miura, H. Itoh, M. Inoue, "Synthesis of 4-Nitrophenyl (2,2,6,6-Tetramethylpiperidin-1-yl) Carbonate (NPTC) for N-Protection of L-Phenylalanine Ethyl Ester," Org. Synth. 2020, 97, 96-124.
DOI: 10.15227/orgsyn.097.0096

Others

伊藤寛晃, "ペプチド系複雑天然物の全合成を基盤とした機能解明・新機能分子創出," 薬事日報 2021, 12432, 19. link
Masayuki Inoue, Kotaro Tokumoto, Takuya Kaji, Hiroaki Itoh, "Design, Construction, and Screening of a One-Bead-One-Compound Library for Discovery of Potent Analogues of Antibiotic Lysocin E," MEDCHEM NEWS 2020, 30 (2), 84-88.
DOI: 10.14894/medchem.30.2_84
伊藤寛晃, 井上将行, "脂質を見分ける天然物," 化学 2015, 70(8), 64-65.

Koichi Hagiwara

Original Papers

2024

T. Kato, K. Hagiwara, M. Inoue, "Generation and Coupling of Radical Species from α-Alkoxy Bridgehead Carboxylic Acid, Selenide, Telluride, Acyl Selenide, and Acyl Telluride," Chem. Pharm. Bull. 2024, 72, 767-771.

DOI: 10.1248/cpb.c24-00441
H. Mutoh, Y. Watanabe, D. Kamakura, K. Hagiwara, M. Inoue, "Unexpected Formation of 11(9→7)-abeo-Steroid Skeleton in Synthetic Studies toward Batrachotoxin," Chem. Pharm. Bull. 2024, in press.

DOI: 10.1248/cpb.c24-00126
H. Asai, K. Hagiwara, M. Inoue, "Enantioselective route to an AE-ring intermediate in the total synthesis of talatisamine," Tetrahedron Lett. 2024, 135, 154903.

DOI: 10.1016/j.tetlet.2023.154903

2023

Y. Watanabe, K. Sakata, D. Urabe, K. Hagiwara, M. Inoue, "Formal Total Synthesis of Batrachotoxin Enabled by Radical and Weix Coupling Reactions," J. Org. Chem. 2023, 88, 17479-17484.
(24/1/4 Selected as Most Read Articles)

DOI: 10.1021/acs.joc.3c02290
Y. Watanabe, H. Morozumi, H. Mutoh, K. Hagiwara, M. Inoue, "Total Synthesis of (−)-Batrachotoxin Enabled by a Pd/Ag-Promoted Suzuki–Miyaura Coupling Reaction," Angew. Chem. Int. Ed. 2023, 62, e202309688.
(Selected as Hot Paper)
(Selected as Top Viewed Article link)

DOI: 10.1002/anie.202309688
T. Shimakawa, S. Nakamura, H. Asai, K. Hagiwara, M. Inoue, "Total Synthesis of Puberuline C," J. Am. Chem. Soc. 2023, 145, 600-609.

(Featured in ChemistryViews)
(Selected as Most Read Articles)
(Featured in Synfacts)
(Featured in Organic Chemistry Highlights)
DOI: 10.1021/jacs.2c11259

2022

T. Nagai, Y. Wang, K. Hagiwara, M. Inoue, "Asymmetric synthesis of evoninic acid," Tetrahedron Lett. 2022, 97, 153747.

DOI: 10.1016/j.tetlet.2022.153747

2021

Y. Wang, T. Nagai, I. Watanabe, K. Hagiwara, M. Inoue, "Total Synthesis of Euonymine and Euonyminol Octaacetate," J. Am. Chem. Soc. 2021, 143, 21037–21047.
(Selected as Most Read Articles)

DOI: 10.1021/jacs.1c11038
H. Mutoh, S. Nakamura, K. Hagiwara, M. Inoue, "Construction of Pentacyclic Limonoid Skeletons via Radical Cascade Reactions," J. Org. Chem. 2021, 86, 6869–6878.

DOI: 10.1021/acs.joc.1c00212

2020

S. Shimizu, K. Hagiwara, H. Itoh, M. Inoue, "Unified Total Synthesis of Five Bufadienolides," Org. Lett. 2020, 22, 8652-8657.
(Selected as Most Read Articles of the month)

DOI: 10.1021/acs.orglett.0c03251
K. Minagawa, D. Kamakura, K. Hagiwara, M. Inoue, "Construction of the ABCE-ring structure of talatisamine via decarboxylative radical cyclization," Tetrahedron 2020, 76, 131385.
(Selected in Editor’s Choice Collection, link)

DOI: 10.1016/j.tet.2020.131385
D. Kamakura, H. Todoroki, D. Urabe, K. Hagiwara, M. Inoue, "Total Synthesis of Talatisamine," Angew. Chem. Int. Ed. 2020, 59, 479-486.
(Featured in Synfacts)
(Featured in Synthesis Workshop Videos, link)
(Selected as Top Downloaded Article link)

DOI: 10.1002/anie.201912737

2016

K. Hagiwara, T. Tabuchi, D. Urabe, M. Inoue, "Expeditious synthesis of the fused hexacycle of puberuline C via radical-based cyclization/translocation/cyclization process," Chem. Sci. 2016, 7, 4372-4378.

DOI: 10.1039/C6SC00671J

2015

K. Hagiwara, M. Iwatsu, D. Urabe, M. Inoue, "N-(2,3,4,5,6-Pentafluorophenyl)maleimide as a Powerful Dienophile in Dearomatizing Diels-Alder Reactions," Heterocycles 2015, 90, 659-672.

DOI: 10.3987/COM-14-S(K)23

Reviews and Accounts

T. Shimakawa, K. Hagiwara, M. Inoue, "Total Synthesis of Talatisamine: Exploration of Convergent Synthetic Strategies," Bull. Chem. Soc. Jpn. 2021, 94, 973-983.

DOI: 10.1246/bcsj.20200400

Book Chapters

Submitted by H. Huang, Z. Xu, G.-J. Deng, Checked by H. Morozumi, K. Hagiwara, M. Inoue, "Synthesis of 2-Phenyl-4,6-bis(trifluoromethyl)pyridine via NH4I/Na2S2O4-Mediated Cyclization of Ketoxime Acetates," Org. Synth. 2023, 100, 248-270.
DOI: 10.15227/orgsyn.100.0248
Submitted by M. Krzeszewski, M. Tasior, M. Grzybowski, D. T. Gryko, Checked by S. Nakamura, K. Hagiwara, M. Inoue, "Synthesis of Tetraaryl-, Pentaaryl-, and Hexaaryl-1,4-dihydropyrrolo[3,2-b]pyrroles," Org. Synth. 2021, 98, 242-262.
DOI: 10.15227/orgsyn.098.0242
Submitted by N. Zhu, W.-M. Wan, H. Bao, Checked by Y. Watanabe, K. Hagiwara, M. Inoue, "Reductive Deuteration of Ketones with Magnesium and D2O for the Synthesis of α-Deutero-o-methyl-benzhydrol," Org. Synth. 2021, 98, 51-67.
DOI: 10.15227/orgsyn.098.0051
Submitted by S. M. Engle, T. R. Kirkner, C. B. Kelly, Checked by S. Shimizu, K. Hagiwara, M. Inoue, "Preparation of 2,4,5,6-Tetra(9H-carbazol-9-yl)isophthalonitrile," Org. Synth. 2019, 96, 455-473.
DOI: 10.15227/orgsyn.096.0455
Submitted by B. J. Simmons, M. Ramirez, N. K. Garg, Checked by T. Shimakawa, K. Hagiwara, M. Inoue, "Facile Reduction of Amides Using Nickel Catalysis: Reduction of 12-Aminododecanolactam," Org. Synth. 2019, 96, 436-454.
DOI: 10.15227/orgsyn.096.0436

Haruka Fujino

Original Papers

2024

J. Taguchi, S. Fukaya, H. Fujino, M. Inoue, "Total Synthesis of Euphorbialoid A," J. Am. Chem. Soc. 2024, 146, 34221-34230.
(24/12/12 Selected as Most Read Articles)
(Featured in Synfacts)
(Featured in Organic Chemistry Highlights)

DOI: 10.1021/jacs.4c14520
Y. Yamada, R. Yoshinaga, Y. Matsui, M. Nagatomo, H. Fujino, M. Inoue, "Et₃Al/Light-Promoted Radical-Polar Crossover Reactions of α-Alkoxyacyl Tellurides," J. Org. Chem. 2024, 89, 11701-11706.

DOI: 10.1021/acs.joc.4c01445

2020

M. Nagatomo, K. Zhang, H. Fujino, M. Inoue, "Et3B/Et2AlCl/O2‐Mediated Radical Coupling Reaction between α‐Alkoxyacyl Tellurides and 2‐Hydroxybenzaldehyde Derivatives," Chem. Asian. J. 2020, 15, 3820-3824.

DOI: 10.1002/asia.202001090
H. Fujino, T. Fukuda, M. Nagatomo, M. Inoue, "Convergent Total Synthesis of Hikizimycin Enabled by Intermolecular Radical Addition to Aldehyde," J. Am. Chem. Soc. 2020, 142, 13227–13234.
(Highlighted in Organic Chemistry Highlights)

DOI: 10.1021/jacs.0c06354

2019

M. Yang, F. Yin, H. Fujino, S. A. Snyder, “The Total Synthesis of Chalctrin,” J. Am. Chem. Soc. 2019, 141, 4515-4520.
DOI: 10.1021/jacs.8b12612

2017

H. Fujino, M. Nagatomo, A. Paudel, S. Panthee, H. Hamamoto, K. Sekimizu, M. Inoue, "Unified Total Synthesis of Polyoxin J, L, and Their Fluorinated Analogues Based on Decarbonylative Radical Coupling Reactions," Angew. Chem. Int. Ed. 2017, 56, 11865-11869.

DOI:10.1002/anie.201706671

2015

M. Nagatomo, H. Nishiyama, H. Fujino, M. Inoue, "Decarbonylative Radical Coupling of α-Aminoacyl Tellurides: Single-Step Preparation of γ-Amino and α,β-Diamino Acids and Rapid Synthesis of Gabapentin and Manzacidin A," Angew. Chem. Int. Ed. 2015, 54, 1537-1541.
(Selected as Hot Paper)

DOI: 10.1002/anie.201410186

Reviews and Accounts

H. Fujino, M. Nagatomo, M. Inoue, "Total Syntheses of Hikosamine and Hikizimycin," J. Org. Chem. 2021, 86, 16220–16230.
(Selected as the cover picture link)

DOI: 10.1021/acs.joc.1c01773

Book Chapters

H. Fujino, M. Inoue, "Convergent Total Synthesis of Hikizimycin: Development of New Radical-Based and Protective Group Strategies," In Modern Natural Product Synthesis, M. Nakada, K. Tanino, K. Nagasawa, S. Yokoshima, Ed.; Springer: Singapore, 2024; pp 127-144.
DOI: 10.1007/978-981-97-1619-7_6
H. Fujino, M. Inoue, "Fragmentation Reactions," Reference Module in Chemistry, Molecular Sciences and Chemical Engineering 2023
DOI: 10.1016/B978-0-323-96025-0.00010-7
Submitted by D. P. Graeff, N. J. Sims, Q. R. Savage, R. K. Jackson, III, A. C. Jackson, D. M. Lawson, M. R. Wixom, J. L. Wood, Checked by Y. Shiga, H. Fujino, M. Inoue, "Preparation of N-Boc-3-methylpyrrole via Anionic Rearrangement," Org. Synth. 2023, 100, 61-83.
DOI: 10.15227/orgsyn.100.0061
Submitted by J. S. Kingsbury, V. L. Rendina, J. S. Burman, B. A. Smolarski, Checked by J. Taguchi, H. Fujino, M. Inoue, "Catalytic Diazoalkane-Carbonyl Homologation: Synthesis of 2,2-Diphenylcycloheptanone and Other Quaternary or Tertiary Arylalkanones and Spirocycles by Ring Expansion," Org. Synth. 2021, 98, 343-362.
DOI: 10.15227/orgsyn.098.0343

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Reviews and Accounts

Koichi Hagiwara

2024 2023 2022 2021 2020 2019 2016 2015

2024 2020 2019 2017 2015