Original Papers


  • 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, xx, xxxx-xxxx.
    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


  • 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
  • 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
  • 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


  • 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


  • 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. Cham.  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


  • Synthetic Study on Acremoxanthone A, Part 2: Model Study on EFG Xanthone Moiety via Nitrile Oxide Cycloaddition–SNAr 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
  • 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


  • 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


  • 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
    Highlighted in Synfacts
  • 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


  • 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.
  • 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


  • 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


  • 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
    Featured by Synfacts
  • 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.
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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


  • 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


  • 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


  • 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


  • 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


  • 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
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    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.
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    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
    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
    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.
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  • 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.
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  • 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.
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  • 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
    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
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  • フローマイクロ合成の最新動向
    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
    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
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  • 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、
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  • 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
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    in Methods and Applications of Cycloaddition Reactions in Organic Syntheses, ed. by Nishiwaki, N. Wiley, New York, 2014, pp.115-134.
  • 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
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  • 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
  • Thiourea, N-[3,5-Bis(trifluoromethyl)phenyl]-N’-[(1R,2R)-2-(dimethylamino)cyclohexyl]-
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  • 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)
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  • 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
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  • 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
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  • 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



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