京都大学大学院薬学研究科薬品合成化学分野

Original Papers

2024

Chromic Properties of Dibenzo[j,l]fluoranthenes Exhibiting Different Resonance Contributions
Kurokawa, K.; Ogawa, N.; Kuroda, Y.; Yamaoka, Y.; Takikawa, H.; Tsubaki, K.; Takasu, K.
Org. Biomol. Chem. 2024, 22, 5306-5313.
DOI: 10.1039/D4OB00750F
Entry into Lithium Ynolates from α,α,α-Tribromomethyl Ketones: Synthesis of Cyclobutenes via the [2 + 2] Cycloaddition with α,β-Unsaturated Carbonyls
Yamaoka, Y.; Imahori, H.; Namioka, M.; Nishina, R.; Kobori, Y.; Ueda, M.; Shindo, M.; Takasu, K.
Org. Lett. 2024, 26, 1986-1901.
DOI: 10.1021/acs.orglett.4c00202
Structure–ATPase Activity Relationship of Rhodamine Derivatives as Potent Inhibitors of P-Glycoprotein CmABCB1
Miwa, S.; Takikawa, H.; Takeuchi, R.; Mizunuma, R.: Matsuoka, K.; Ogawa, H.; Kato, H.; Takasu, K.
ACS Med. Chem. Lett. 2024, 15, 287-293.
DOI: 10.1021/acsmedchemlett.3c00526
Synthesis of mesoionic triazolones via a formal [3+2] cycloaddition between 4-phenyl-1,2,4-triazoline-3,5-dione and alkynes
Kuroda, Y.; Krell, M.; Kurokawa, K.; Takasu, K.
Chem. Commun. 2024, 60, 1719-1722.
DOI: 10.1039/D3CC05088B

2023

Sequential Bromination/Dearomatization Reactions of 2-Methoxyphenols en route to Bromo-Substituted ortho-Quinonemonoacetals
Hayashi, S.; Takasu, K.; Takikawa, H.
Synlett 2023, 35, 474-478.
DOI: 10.1055/s-0041-1738450
Rotaxane Synthesis by an End-Capping Strategy via Swelling Axle-Phenols
Fujimura, K.; Ueda, Y.; Yamaoka, Y.; Takasu, K.; Kawabata, T.
Angew. Chem. Int. Ed. 2023, 63, e202303078.
DOI: 10.1002/anie.202303078
An Iridium/Aluminum Cooperative Strategy for the β-C(sp3)–H Borylation of Saturated Cyclic Amines
Kuroda, Y.; Park, K.; Shimazaki, Y.; Zhong, R.-L.; Sakaki, S.; Nakao, Y.
Angew. Chem. Int. Ed. 2023, 62, e202300704.
DOI: 10.1002/anie.202300704
Efficient Synthesis of Medium-sized Nitrogen Heterocycles by Brønsted Acid-Catalyzed Cyclization of Ene-ynamides
Yamaoka, Y.; Takeuchi, N.; Yamada, K.; Takasu, K.
Asian J. Org. Chem. 2023, 12, e202300145.
DOI: 10.1002/ajoc.202300145
Intramolecular Ynamide–Benzyne (3+2) Cycloadditions
Tawatari, T.; Kato, R.; Kudo, R.; Takasu, K.; Takikawa, H.
Angew. Chem. Int. Ed. 2023, 62, e202300907.
DOI: 10.1002/anie.202300907
京都大学プレスリリース
Synthesis of γ-Aryl Medium-sized Cyclic Enones by a domino 4π-Electrocyclic Reaction—Heck–Matsuda Arylation Sequence at Ambient Temperature
Ito, T.; Takeuchi, N.; Yamaoka, Y.; Takikawa, H.; Takasu, K.
Synthesis 2023, 34, 1275-1279.
DOI: 10.1055/a-2024-4675

2022

Lewis Acid-Catalyzed Diastereoselective Domino Reaction of Ene-Ynamide with Trimethylsilyl Cyanide to Construct Spiroindolines
Yamaoka, Y.; Yamasaki, D.; Kajiwara, D.; Shinosaki, M.; Yamada, K.; Takasu, K.
Org. Lett. 2022, 24, 4389-4393.
DOI: 10.1021/acs.orglett.2c01607
Enhanced Molecular Recognition through Substrate–Additive Complex Formation in N-Heterocyclic-Carbene-Catalyzed Kinetic Resolution of α-Hydroxythioamides
Wang, Y.; Yamauchi, A.; Hashimoto, K.; Fujiwara, T.; Inokuma, T.; Mitani, Y.; Ute, K.; Kuwano, S.; Yamaoka, Y.; Takasu, K.; Yamada, K.
ACS Catal. 2022, 12, 6100-6107.
DOI: 10.1021/acscatal.2c01579
Intramolecular Propargylic Ene Reaction of Benzyne en Route to Highly Functionalized Allenes and Allenamides
Tawatari, T.; Kato, R.; Takasu, K.; Takikawa, H.
Synthesis 2022, 54, 4979-4988.
DOI: 10.1055/a-1826-2545
AI-Driven Synthetic Route Design Incorporated with Retrosynthesis Knowledge
Ishida, S.; Terayama, K.; Kojima, R.; Takasu, K.; Okuno, Y.
J. Chem. Inf. Model. 2022, 62, 1357-1367.
DOI: 10.1021/acs.jcim.1c01074
Total Synthesis of Cryptopleurine and Its Analogues
Yamaoka, Y.; Yamakawa, T.; Tateishi, K.; Takasu, K.
Synthesis 2022, 54, 2415-2422.
DOI: 10.1055/a-1730-8628
Catalytic Substrate-Selective Silylation of Primary Alcohols via Remote Functional-Group Discrimination
Hashimoto, H.; Ueda, Y.; Takasu, K.; Kawabata, T.
Angew. Chem. Int. Ed. 2022, 61, e202114118.
DOI: 10.1002/anie.202114118

2021

2-(Chlorodiisopropylsilyl)-6-(trimethylsilyl)phenyl triflate: a modified platform for intramolecular benzyne cycloadditions
Tawatari, T.; Takasu, K.; Takikawa, H.
Chem. Commun. 2021, 57, 11863-11866.
DOI: 10.1039/D1CC05264K
Oxidative β-Cleavage of Fused Cyclobutanols Leading to Hydrofuran-Fused Polycyclic Aromatic Compounds
Kinouchi, H.; Sugimoto, K.; Yamaoka, Y.; Takikawa, H.; Takasu, K.
J. Org. Chem. 2021, 86, 12615-12622.
DOI: 10.1021/acs.joc.1c01108
The Rationale for Stereoinduction in Conjugate Addition to Alkylidenemalonates Bearing a Menthol-derived Chiral Auxiliary
Yamada, K.; Fujiwara, S.; Inokuma, T.; Sugano, M.; Yamaoka, Y.; Takasu, K.
Tetrahedron 2021, 91, 132220.
DOI: 10.1016/j.tet.2021.132220
Mechanistic Support for Intramolecular Migrative Cyclization of Propargyl Sulfones Provided by Catalytic Asymmetric Induction with a Chiral Counter Cation Strategy
Yamasaki, K.; Yamauchi, A.; Inokuma, T.; Miyakawa, Y.; Wang, Y.; Oriez, R.; Yamaoka, Y.; Takasu, K.; Tanaka, M.; Kashiwada, Y.; Yamada, K.
Asian J. Org. Chem. 2021, 10, 1828-1834.
DOI: 10.1002/ajoc.202100274
Synthesis of Lactone-fused Cyclopropanes by Ring Contractive a-Ketol Rearrangement of Ketal-fused Cyclobutanones
Takasu, K.; Shigenaga, K.; Shimoda, K.; Takikawa, H.; Yamaoka, Y.
Heterocycles 2021, 103, 177-182.
DOI: 10.3987/COM-20-S(K)6

2020

Synthetic Study on Acremoxanthone A, Part 2: Model Study on EFG Xanthone Moiety via Nitrile Oxide Cycloaddition–S_NAr Sequence
Nakakohara, H.; Hirano, Y.; Ohmori, K.; Takikawa, H.; Suzuki, K.
Synlett 2020, 32, 423-428.
DOI: 10.1055/a-1303-5613
Total Synthesis of (−)-Sigillin A: A Polychlorinated and Polyoxygenated Natural Product
Yamaoka, Y.; Nakayama, T.; Kawai, S.; Takasu, K.
Org. Lett. 2020, 22, 7721-7724.
DOI: 10.1021/acs.orglett.0c02930
CompRet: a comprehensive recommendation framework for chemical synthesis planning with algorithmic enumeration
Shibukawa, R.; Ishida, S.; Yoshizoe, K.; Wasa, K.; Takasu, K.; Okuno, Y.; Terayama, K.; Tsuda, K.
J. Cheminf. 2020, 12, 52.
DOI: 10.1186/s13321-020-00452-5
Synthetic Study on Lactonamycins, Part 2: Stereoselective Access to ABCD-Ring System
Takikawa, H.; Murata, K.; Sato, S.; Kawada, T.; Nakakohara, H.; Ohmori, K.; Suzuki, K.
Synlett 2020, 31, 1623-1628.
DOI: 10.1055/s-0040-1707198
Helical Nanographenes Embedded with Contiguous Azulene Units
Ogawa, N.; Yamaoka, Y.; Takikawa, H.; Yamada, K.; Takasu, K.
J. Am. Chem. Soc. 2020, 142, 13322-13327.
DOI: 10.1021/jacs.0c06156
京都大学プレスリリース
 Chem-Stationスポットライトリサーチ
Intramolecular Benzyne–Phenolate [4+2] Cycloadditions
Takikawa, H.; Nishii, A.; Takiguchi, H.; Yagishita, H.; Tanaka, M.; Hirano, K.; Uchiyama, M.; Ohmori, K.; Suzuki, K.
Angew. Chem. Int. Ed. 2020, 59, 12440-12444.
DOI: 10.1002/anie.202003131

2019

Prediction and Interpretable Visualization of Retrosynthetic Reactions using Graph Convolutional Networks
Ishida, S.; Terayama, K.; Kojima, R.; Takasu, K.; Okuno, Y.
J. Chem. Inf. Model. 2019, 59, 5026-5033.
DOI: 10.1021/acs.jcim.9b00538
Synthesis of Polycyclic Spirocarbocyles via Acid-Promoted Ring-Contraction/Dearomative Ring-Closure Cascade of Oxapropellanes
Ogawa, N.; Yamaoka, Y.; Takikawa, H.; Takasu, K.
Org. Lett. 2019, 21, 7563-7567.
DOI: 10.1021/acs.orglett.9b02835
Synthesis of Dibenzoxazonines by Domino (2+2) Cycloaddition—4π Electrocyclic Ring Opening Reaction of Cyclic Imines with Ynamides
Takasu, K.; Tsustumi, M.; Ito, T.; Takikawa, H.; Yamaoka, Y.
Heterocycles, 2020, 101, 423-428.
DOI: 10.3987/COM-19-S(F)39
Total Syntheses of Allelopathic 4-Oxyprotoilludanes, Melleolides and Echinocidins
Shimoda, K.; Yamaoka, Y.; Yoo, D.; Yamada, K.; Takikawa, H.; Takasu, K.
J. Org. Chem. 2019, 84, 11014-11024.
DOI: 10.1021/acs.joc.9b01589
Synthesis of Functionalized Medium-Sized trans-Cycloalkenes by 4π Electrocyclic Ring Opening– Alkylation Cascade
Ito, T.; Tsutsumi, M.; Yamada, K.; Takikawa, H.; Yamaoka, Y.; Takasu, K.
Angew. Chem. Int. Ed. 2019, 58, 11836-11840.
DOI: 10.1002/anie.201906665
Rapid Assembly of Protoilludane Skeleton through Tandem Catalysis: Total Synthesis of Paesslerin A and Its Structural Revision
Mogi, Y.; Inanaga, K.; Tokuyama, H.; Ihara, M.; Yamaoka, Y.; Yamada, K.; Takasu, K.
Org. Lett. 2019, 21, 3954–3958.
DOI: 10.1021/acs.orglett.9b01089
Asymmetric Formal Synthesis of (+)-Catharanthine via Desymmetrization of Isoquinuclidine
Kono, M.; Harada, S.; Nozaki, T.; Hashimoto, Y.; Murata, S.; Gröger, H.; Kuroda, Y.; Yamada, K.; Takasu, K.; Hamada, Y.; Nemoto, T.
Org. Lett. 2019, 21, 3750–3754.
DOI: 10.1021/acs.orglett.9b01198
2-Bromo-6-(chlorodiisopropylsilyl)phenyl tosylate as an efficient platform for intramolecular benzyne–diene [4+2] cycloaddition
Nishii, A.; Takikawa, H.; Suzuki, K.
Chem. Sci. 2019, 10, 3840-3845.
DOI: 10.1039/c8sc05518a
Optical Resolution via Catalytic Generation of Chiral Auxiliary
Kiyama, H.; Inokuma, T.; Kuroda, Y.; Yamaoka, Y.; Takasu, K.; Yamada, K.
Tetrahedron Lett. 2019, 60, 175-177.
DOI: 10.1016/j.tetlet.2018.12.006

2018

Silyl enol etherification by a Tf₂NH/amine co-catalytic system for minimizing hazardous waste generation
Kurahashi, K.; Yamaoka, Y.; Takemoto, Y.; Takasu, K.
React. Chem. Eng. 2018, 3, 626-630.
DOI: 10.1039/C8RE00039E
Synthesis and Properties of Tribenzocarbazoles via an Acid-Promoted Retro (2+2)-Cycloaddition of Azapropellanes
Ogawa, N.; Yamaoka, Y.; Takikawa, H.; Tsubaki, K.; Takasu, K.
J. Org. Chem. 2018, 83, 7994-8002.
DOI: 10.1021/acs.joc.8b00870
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Total Synthesis of Phenanthroquinolizidine Alkaloid Cryptopleurine and Phenanthroindolizidine Alkaloid Tylophorine
Yamaoka, Y.; Taniguchi, M.; Yamada, K.; Takasu, K.
Heterocycles 2018, 97, 292-305.
DOI: 10.3987/COM-18-S(T)19
Total Synthesis of Bis-anthraquinone Antibiotic BE-43472B
Yamashita, Y.; Hirano, Y.; Takada, A.; Takikawa, H.; Suzuki, K.
Synthesis 2018, 50, 2490-2515.
DOI: 10.1055/s-0037-1610136

2017

Synthesis of Multi-substituted Cyclobutenes: Cyclic Strategy for (2+2) Cycloaddition of Ketene Silyl Acetals with Propiolates
Yamaoka, Y.; Ueda, M.; Yamashita, T.; Shimoda, K.; Yamada, K.; Takasu, K.
Tetrahedron Lett. 2017, 58, 2944-2947.
DOI: 10.1016/j.tetlet.2017.06.039
Synthesis of π-Extended Fluoranthenes via a KHMDS-Promoted Anion and Radical Reaction Cascade
Ogawa, N.; Yamaoka, Y.; Yamada, K.; Takasu, K.
Org. Lett. 2017, 19, 3327-3330.
DOI: 10.1021/acs.orglett.7b01538
Synthesis and biological evaluation of steroidal derivatives bearing a small ring as vitamin D receptor agonists
Arichi, N.; Fujiwara, S.; Ishizawa, M.; Makishima, M.; Hua, D. H.; Yamada, K.; Yamaoka, Y.; Takasu, K.
Bioorg. Med. Chem. Lett. 2017, 27, 3408-3411.
DOI: 10.1016/j.bmcl.2017.05.089
Site-selective benzoin-type cyclization of unsymmetrical dialdoses catalyzed by N-heterocyclic carbenes for divergent cyclitol synthesis
Kang, B.; Wang, Y.; Kuwano, S.; Yamaoka, Y.; Takasu, K.; Yamada, K.
Chem. Commun. 2017, 53, 4469-4472.
DOI:10.1039/C7CC01191A
Total Synthesis of (-)-Histrionicotoxin through a Stereoselective Radical Translocation-Cyclization Reaction
Sato, M.; Azuma, H.; Daigaku, A.; Sato, S.; Takasu, K.; Okano, K.; Tokuyama, H.
Angew. Chem. Int. Ed. 2017, 56, 1087-1091.
DOI: 10.1002/anie.201609941
Phosphine-Promoted Migrative Cyclization of Sulfonylalkynol and Sulfonylalkynamide for the Synthesis of Oxa- and Azacycles
Wang, Y.; Oriez, R.; Oh, S.; Miyakawa, Y.; Yamaoka, Y.; Takasu, K.; Yamada, K.
Heterocycels, 2017, 95, 314-321.
DOI: 10.3987/COM-16-S(S)22

2016

Use of a Catalytic Chiral Leaving Group for Asymmetric Substitutions at sp³-Hybridized Carbon Atoms: Kinetic Resolution of β-Amino Alcohols by p-Methoxybenzylation
Kuroda, Y.; Harada, S.; Oonishi, A.; Kiyama, H.; Yamaoka, Y.; Yamada, K.; Takasu, K.
Angew. Chem. Int. Ed. 2016, 55, 13137-13141.
DOI: 10.1002/anie.201607208
Desymmetrization of acid anhydride with asymmetric esterification catalyzed by chiral phosphoric acid
Yamada, K.; Oonishi, A.; Kuroda, Y.; Harada, S.; Yamaoka, Y.; Kiyama, H.; Takasu, K.
Tetrahedron Lett. 2016, 57, 4098-4100.
DOI: 10.1016/j.tetlet.2016.07.093
Striking Difference between Succinimidomethyl and Phthalimidomethyl Radicals in Conjugate Addition to Alkylidenemalonate Initiated by Dimethylzinc
Yamada, K.; Matsumoto, Y.; Fujii, S.; Konishi, T.; Yamaoka, Y.; Takasu, K.
J. Org. Chem. 2016, 81, 3809-3817.
DOI: 10.1021/acs.joc.6b00485
Oxa- and Azacycle Formation via Migrative Cyclization of Sulfonylalkynol and Sulfonylalkynamide with N-Heterocyclic Carbene
Wang, Y.; Oriez, R.; Kuwano, S.; Yamaoka, Y.; Takasu, K.; Yamada, K.
J. Org. Chem. 2016, 81, 2652-2664.
DOI: 10.1021/acs.joc.6b00182

2015

An Arylative Ring Expansion Cascade of Fused Cyclobutenes via Short-Lived Intermediates with Planar Chirality
Arichi, N.; Yamada, K.; Yamaoka, Y.; Takasu, K.
J. Am. Chem. Soc. 2015, 137, 9579-9682.
DOI: 10.1021/jacs.5b06576
Asymmetric Total Synthesis of Tylophorine via a Formal [2+2] Cycloaddition Followed by Migrative Ring Opening of a Cyclobutane
Yamaoka, Y.; Taniguchi, M.; Yamada, K.; Takasu, K.
Synthesis 2015, 47, 2819-2825.
DOI: 10.1055/s-0034-1380430
The 10 most popular articles of the last month.
Organocatalytic Activation of the Leaving Group in the Intramolecular Asymmetric SN2′ Reaction
Kuroda, Y.; Harada, S.; Oonishi, A.; Yamaoka, Y.; Yamada, K.; Takasu, K.
Angew. Chem. Int. Ed. 2015, 54, 8263-8266.
DOI: 10.1002/anie.201502831
Featured by Synfacts, selected as Synfact of the month, Featured by Advances in Engineering.
The Development of a Brønsted Acid-promoted Ene-Ynamide Cyclization toward the Total Syntheses of Marinoquinolines A and C, and Aplidiopsamine
A, Yamaoka, Y.; Yoshida, T.; Shinozaki, M.; Yamada, K.; Takasu, K.
J. Org. Chem. 2015, 80, 957-964.
DOI: 10.1021/jo502467m
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Synthesis of Steroidal Derivatives Bearing a Small Ring Using a Catalytic [2+2] Cycloaddition and a Ring-Contraction Rearrangement
Arichi, N.; Hata, K.; Takemoto, Y.; Yamada, K.; Yamaoka, Y.; Takasu, K.
Tetrahedron 2015, 71, 233-243.　
DOI: 10.1016/j.tet.2014.11.065
Contiguous Radical Pivaloyloxymethylation-Directed C(sp³)-H Iodination of N-Tosyl Cycloalkanecarbaldimine
Fujii, S.; Nakano, M.; Yamaoka, Y.; Takasu, K.; Yamada, K.; Tomioka, K.
Tetrahedron Lett. 2015, 56, 3086-3089.
DOI: 10.1016/j.tetlet.2014.11.105
Hydrostannylation-Cross-Coupling Strategy for Stereoselective Synthesis of Alkylidenemalonates and Related α,β-Unsaturated Esters
Fujiwara, S.; Cadou, R.; Yamaoka, Y.; Takasu, K.; Yamada, K.
Eur. J. Org. Chem. 2015, 1264-1272.
DOI: 10.1002/ejoc.201403429
Synthetic Studies toward Penitrem E: Enantiocontrolled Construction of B-E Rings
Yoshii, Y.; Otsu, T.; Hosokawa, T.; Takasu, K.; Okano, K.; Tokuyama, K.
Chem. Commun. 2015, 51, 1070-1073.
DOI:10.1039/C4CC08505A
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N-Heterocyclic Carbene-Catalyzed Benzoin Strategy for Divergent Synthesis of Cyclitol Derivatives from Alditols
Kang, B.; Suto, T.; Wang, Y.; Kuwano, S.; Yamaoka, Y.; Takasu, K.; Yamada, K.
Adv. Synth. Catal. 2015, 357, 131-147.
DOI: 10.1002/adsc.201400712

2014

Stereocontrolled Total Synthesis And Biological Evaluation of (-)- And (+)-Petrosin and Its Derivatives
Toya, H.; Satoh, T.; Okano, K.; Takasu, K.; Ihara, M.; Takahashi, A.; Tanaka, H.; Tokuyama, H.
Tetrahedron 2014, 70, 8129-8141.
DOI: 10.1016/j.tet.2014.08.009
Radical Amidomethylation of Imines
Fujii, S.; Konishi, T.; Matsumoto, Y.; Yamaoka, Y.; Takasu, K.; Yamada, K.
J. Org. Chem. 2014, 79, 8128-8133.
DOI: 10.1021/jo501332j
Equilibration of the EtAlCl2-Catalyzed [2 + 2] Cycloaddition of Silyl Enol Ethers: Diastereoselectivity Switch in the Synthesis of Fused Cyclobutanes
Hata, K.; Arichi, N.; Yamaoka, Y.; Yamada, K.; Takemoto, Y.; Takasu, K.
Asian J. Org. Chem. 2014, 3, 706-710.
DOI: 10.1002/ajoc.201402042
Synthesis of Functionalized Polycyclic Aromatic Compounds via a Formal [2+2]-cycloaddition
Nagamoto, Y.; Yamaoka, Y.; Fujimura, S.; Takemoto, Y.; Takasu, K.
Org. Lett. 2014, 16, 1008-1011.
DOI: 10.1021/ol403757e

2013

Enhanced Rate and Selectivity by Carboxylate Salt as a Basic Co-catalyst in Chiral N-Heterocyclic Carbene-Catalyzed Asymmetric Acylation of Secondary Alcohols
Kuwano, S.; Harada, S.; Kang, B.; Raphael, O.; Yamaoka, Y.; Takasu, K.; Yamada, K.
J. Am. Chem. Soc. 2013, 135, 11485-11488.
DOI: 10.1021/ja4055838
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Kinetic resolution of secondary alcohols catalyzed by chiral phosphoric acids
Harada, S.; Kuwano, S.; Yamaoka, Y.; Yamada, K.; Takasu, K.
Angew. Chem. Int. Ed. 2013, 52, 10227-10230.
DOI: 10.1002/anie.201304281
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Synthesis of 2,3,4,5-Tetra-substituted Pyrroles via a Base-Promoted Double Michael Reaction of Oxime-enoates with Nitroolefins
Kuroda, Y.; Imaizumi, K.; Yamada, K.; Yamaoka, Y.; Takasu, K.
Tetrahedron Lett. 2013, 54, 4073-4075.
DOI: 10.1016/j.tetlet.2013.05.100
Selective Synthesis of Poly-Substituted Dihydroquinolines and α,β-Unsaturated Amidines by A Catalytic Reaction of Ynamides with Ketimines
Kuroda, Y.; Shindoh, N.; Takemoto, Y.; Takasu, K.
Synthesis 2013, 45, 2318-2326.
DOI: 10.1055/s-0033-1339191
Critical profiles of chiral diether-mediated asymmetric conjugate aminolithiation of enoate with lithium amide as a key to the total synthesis of (-)-kopsinine
Harada, S.; Sakai, T.; Takasu, K.; Yamada, K.; Tomioka, K.
Tetrahedron 2013, 69, 3264-3273.
DOI: 10.1016/j.tet.2013.02.035
pH-sensitive DNA cleaving agents: in situ activation by ring contraction of benzo-fused cyclobutanols
Nagamoto, Y.; Hattori, A.; Kakeya, H.; Takemoto, Y.; Takasu, K.
Chem. Commun. 2013, 49, 2622-2624.
DOI: 10.1039/c3cc39246e
Study of Ring-Opening Reaction of Spiro[5.2]octenes with Aqueous Hydro-halic Acid: Substituent Effect on the Regioselectivity
Nagamoto, Y.; Takemoto, Y.; Takasu, K.
Synlett 2013, 24, 120-124.
DOI: 10.1055/s-0032-1317745

2012

Total Synthesis of (+)-trans-Dihydronarciclasine Utilizing Asymmetric Conjugate Addition
Yamada, K.; Mogi, Y.; Mohamed, M. A.; Takasu, K.; Tomioka, K.
Org. Lett. 2012, 14, 5868-5871.
DOI: 10.1021/ol302757y
Total Synthesis of (-)-Kopsinine by an Asymmetric One-Pot [N+2+3] Cyclization
Harada, S.; Sakai, T.; Takasu, K.; Yamada, K.; Tomioka, K.
Chem. Asian J. 2012, 7, 2196-2198.
DOI: 10.1002/asia.201200575
General Entry to Asymmetric One-Pot [N + 2 + n] Cyclization for the Synthesis of Three- to Seven-Membered Azacycloalkanes
Harada, S.; Sakai, T.; Takasu, K.; Yamada, K.; Tomioka, K.
J. Org. Chem. 2012, 77, 7212-7222. Featured by Synfacts
DOI: 10.1021/jo301495a
Facile Isomerization of Silyl Enol Ethers Catalyzed by Triflic Imide and Its Application to One-pot Isomerization-(2 + 2) Cycloaddition
Inanaga, K.; Ogawa, Y.; Nagamoto, Y.; Daigaku, A.; Tokuyama, H.; Takemoto, Y.; Takasu, K.
Beilstein J. Org. Chem. 2012, 8, 658-661.
DOI: 10.3762/bjoc.8.73
Room-temperature, acid-catalyzed [2+2] cycloadditions: Suppression of side reactions by using a flow microreactor system
Kurahashi, K.; Takemoto, Y.; Takasu, K.
ChemSusChem 2012, 5, 270-273.
DOI: 10.1002/cssc.201100373

2011

Formal (3 + 3) Cycloaddition of Silyl Enol Ethers Catalyzed by Trifric Imide: Domino Michael Addition-Claisen Condensation Accompanied with Isomerization of Silyl Enol Ethers
Azuma, T.; Takemoto, Y.; Takasu, K.
Chem. Pharm. Bull. 2011, 59, 1190-1193.
DOI: 10.1248/cpb.59.1190
Catalyst-Controlled Torquoselectivity Switch in the 4π Ring-Opening Reaction of 2-Amino-2-azetines Giving β-Substituted α,β-Unsaturated Amidines
Shindoh, N.; Kitaura, K.; Takemoto, Y.; Takasu, K.
J. Am. Chem. Soc. 2011, 133, 8470-8473.
DOI: 10.1021/ja202576e
Unprecedented Synthesis of N,N-Divinylamines by Tf₂NH-Catalyzed Reaction of Ynamide with Ketimine
Shindoh, N.; Takemoto, Y.; Takasu, K.
Heterocycles 2011, 82, 1133-1136.
DOI: 10.3987/COM-10-S(E)87
Gold(I)-Catalyzed Polycyclizations of Polyenyne-Type Anilines Based on Hydroamination and Consecutive Hydroarylation Cascade
Hirano, K.; Inaba, Y.; Takasu, K.; Oishi, S.; Takemoto, Y.; Fujii, N.; Ohno, H.
J. Org. Chem. 2011, 76, 9068-9080.
DOI: 10.1021/jo2018119

Reviews

脱芳香化された多環性芳香族ポリケチド天然物の合成戦略
瀧川紘，鈴木啓介，
有機合成化学協会誌，2019, 77(1), 13-25.
DOI: 10.5059/yukigoseikyokaishi.77.13
Aryne-Based Strategy in Total Synthesis of Naturally-Occurring Polycyclic Compounds
Takikawa, H.; Nishii, A.; Sakai, T.; Suzuki, K.
Chem. Soc. Rev. 2018, 47, 8030-8056.
DOI: 10.1039/c8cs00350e
Top 5% of highly cited authors with RSC journals in 2019
ポリケチド系多環性化合物の全合成における試行錯誤
瀧川紘，
有機合成化学協会誌，2018, 76(5), 478-481.
DOI: 10.5059/yukigoseikyokaishi.76.478
キラルリン酸による触媒的不斉置換反応およびアシル化反応への展開
黒田悠介，原田慎吾，山田健一，高須清誠，
有機合成化学協会誌，2018, 76(4), 325-335.
DOI: 10.5059/yukigoseikyokaishi.76.325
Synthesis of Azaheterocycles and Related Molecules by Tf₂NH-Catalyzed Cycloadditions
Shindo, N.; Takasu, K.
Heterocycles 2018, 96, 195-218.
DOI: 10.3987/REV-17-875

形式的[2+2]環化反応を用いた多環芳香族炭化水素の合成とその応用 (Efficient Synthesis of Polyaromatic Hydrocarbon via a Formal [2＋2] Cycloaddition)
山岡庸介(Yousuke Yamaoka)
Yakugaku Zasshi, 2016, 136, 1517-1523.
DOI: 10.1248/yakushi.16-00202
π-Delocalized Lipophilic Quaternary Cations as new Candidates for Antimalarial, Antitrypanosomal and Antileishmanial Agents: Synthesis, Evaluation of Antiprotozoal Potency and Insight of their Action Mechanism
Takasu, K.
Chem. Pharm. Bull. 2016, 64(7), 656-667.
DOI: 10.1248/cpb.c16-00234
Synthesis of Multisubstituted Silyloxy-based Donor-Acceptor Cyclobutanes by an Acid-Catalyzed [2+2] Cycloaddition
Takasu, K.
Israel J. Chem. 2016, 56(6-7), 488-498.
DOI: 10.1002/ijch.201500096
トリフリックイミドのオート・タンデム触媒作用を利用する有機合成
高須清誠，
有機合成化学協会誌，2014, 72(7), 770-780.
DOI: 10.5059/yukigoseikyokaishi.72.770
軸性不斉をもつアミジンの触媒的不斉合成法の開発とキラル合成素子としての活用
高須清誠,
薬学研究の進歩, 2011, 31-36.

Books

フローマイクロ合成の最新動向
高須清誠著、ファインケミカル合成プロセス
シーエムシー出版, 2021, pp.102-110. ISBN 978-4-7813-1615-4
スタンダード薬学シリーズII-8　薬学研究, 日本薬学会編
藤多哲朗、高須清誠著、人とのつながりが結実して誕生した新薬－冬虫夏草を起源とする多発性硬化症治療薬フィンゴリモド
東京化学同人, 2017, pp.36-44. ISBN 9784807917228
くすりをつくる研究者の仕事京都大学大学院薬学研究科編
高須清誠、第２章　薬を合成する－炭素の錬金術師
化学同人、2017, pp.35-62.　ISBN 9784759819311.
スタンダード薬学シリーズII -3　化学系薬学　II.
伊藤喬、石崎幸、石塚忠男、橘高敦、高須清誠編
東京化学同人, 2016.
スタンダード薬学シリーズII -3　化学系薬学　III.
伊藤喬、石崎幸、石塚忠男、橘高敦、高須清誠、供田洋、森田博史編、
東京化学同人, 2016.
スタンダード薬学シリーズII- 3　化学系薬学　I. 化学物質の性質と反応
伊藤喬、石崎幸、石塚忠男、橘高敦、高須清誠編、第１章化学結合と分子、
東京化学同人, 2015, pp.2-14.
ウォーレン有機合成－逆合成からのアプローチ－（翻訳）
Warren, S. and Wyatt, P. 著、柴崎正勝、橋本俊一　監訳、金井求、木越英夫、高須清誠、松永茂樹　訳、
東京化学同人，2014, pp. 202-279.　
Catalytic [2+2] Cycloaddition of Silyl Enol Ethers
Yamaoka, Y. and Takasu, K.
in Methods and Applications of Cycloaddition Reactions in Organic Syntheses, ed. by Nishiwaki, N. Wiley, New York, 2014, pp.115-134.
DOI:10.1002/9781118778173.ch04
Reactions involving an α,β-Unsaturated Carbonyl Compound as Electrophilic Component with [2+2] Cycloaddition as the Key Step
Takasu, K.
in Science of Synthesis (Multicomponent Reactions), 2013, Thieme, pp.195-210.
Heterogeneous Reactions
Takasu, K.
in Microreactors in Organic Chemistry and Catalysis, 2nd edition, ed by Wirth, T. Wiley-VCH, Weinheim, 2013, pp. 151-196.
原虫オルガネラの固有環境認識を基盤とした抗マラリア活性物質の創製
高須清誠，
ナノバイオ技術と創薬研究（佐治英郎ら編），メディカルドゥ，2012、pp.72-77.
Thiourea, N-[3,5-Bis(trifluoromethyl)phenyl]-N’-[(1R,2R)-2-(dimethylamino)cyclohexyl]-
Takasu, K.; Takemoto, Y.
Encyclopedia of Reagents for Organic Synthesis (Wiley), 2012, 1-4.
DOI: 10.1002/047084289X.rn01414

Patents

高須清誠、奥野恭史、瀬木恵里、原貴史、藤村駿、山本佳宏、金井千里、吉川達也、閨正博、河野晋哉「ピペラジン誘導体およびその用途」 WO 2014/024993（特願JP2012-177572）
高須清誠，竹本佳司，倉橋慧「シリルエノール類の製造法」特願2010-48290
高須清誠，井原正隆，稲永風人「多置換シクロブタン及び多置換シクロブテン化合物の製造方法」特開2007-119488
井原正隆，高須清誠，Pudhom Khanitha，北口博司，川上雅之，佐藤幸藏「アザロダシアニン化合物を有効成分として含有する原虫感染症治療剤」 WO2006/137258 (特願JP2005-50064)
井原正隆，高須清誠，北口博司，川上雅之，佐藤幸藏「フェノキサジニウム化合物を有効成分とする原虫感染症治療剤」 WO2006/087935 (特願JP2005-41238)
高須清誠，井原正隆，稲永風人「多置換シクロブタン及び多置換シクロブテン化合物の製造方法」 WO2006/009119 (特願JP2006-529195)
井原正隆，高須清誠，Pudhom Khanitha，北口博司，川上雅之，佐藤幸藏「原虫寄生感染症の予防又は治療用医薬組成物」特開2006-104116
井原正隆，高須清誠，Pudhom Khanitha，北口博司，川上雅之，佐藤幸藏「抗トリパノソーマ剤」特開2006-104115，未請求
井原正隆，高須清誠「マラリア増殖阻害に関与するタンパク質」特開2006-67867
井原正隆，高須清誠，西田直子「置換ピペリジン及びその製法」特開JP2005-75785
井原正隆，高須清誠，寺内広毅，関田節子，高橋真理衣「リーシュマニア治療剤」特開JP2004-331545
井原正隆，高須清誠，寺内広毅「メロシアニン系色素化合物及びロダシアニン系色素化合物のコンビナトリアル製造方法」特開JP2004-137271
井原正隆，高須清誠，伊上博史，綿矢有佑，金惠淑「マラリア感染診断剤およびマラリア原虫染色剤」特開JP2004-144526
井原正隆，高須清誠，綿矢有佑，金惠淑「ロダシアニン系色素化合物を含有する抗マラリア剤」特開JP2003-34642
井原正隆，高須清誠，綿矢有佑，金惠淑「四環性複素化合物を含有する抗マラリア剤」特開JP2003-34641
井原正隆，高須清誠，綿矢有佑，金惠淑「ロダシアニン色素化合物を含有する抗マラリア剤」特開JP2003-34640
井原正隆，高須清誠，綿矢有佑，金惠淑「抗マラリア活性を有する新規化合物」特開JP2001-24755