Original Papers

(77) Auto-Tandem Catalysis in Synthesis of Substituted Quinolines from Aldimines and Electron-rich Olefins: Cascade Povarov-Hydrogen Transfer Reaction
　　N. Shindoh, H. Tokuyama, Y. Takemoto, K. Takasu
　　J. Org. Chem., submitted for publication

(76) Triflic Imide Catalyzed (3+2) Cycloaddition of Aldimines with alpha-,alpha-Dimethylallylsilane
　　N. Shindoh, H. Tokuyama, Y. Takemoto, K. Takasu
　　Heterocycles, submitted for publication

(75) Mild Debenzylation of Aryl Benzyl Ether with BCl₃ in the Presence of Pentamethylbenzene as a Non-Lewis-Basic Cation Scavenger
　　K. Okano, K. Okuyama, T. Fukuyama, H. Tokuyama
　　Synlett., accepted for publication

(74) (2 + 2) Cycloaddition Reaction of Alkyl Enol Ethers with Acrylates by in situ Generated Silyl Trifric Imide Catalyst
　　K. Takasu, Y. Miyakawa, M. Ihara, H. Tokuyama
　　Chem. Pharm. Bull, accepted for publication

(73) Synthesis of Eudistomin C and E: Improved Preparation of the Indole Unit
　　H. Yamagishi, K. Matsumoto, K. Iwasaki, T. Miyazaki, S. Yokoshima, H. Tokuyama, T. Fukuyama
　　Org. Lett., 10, 2369-2372 (2008)

(72) Total Synthesis of (-)-Kainic Acid via Intramolecular Michael Addition: A Second-Generation Route
　　H. Sakaguchi, H. Tokuyama, T. Fukuyama
　　Org. Lett., 10, 1711-1714 (2008)

(71) Total Synthesis of (+)-Yatakemycin
　　K. Okano, H. Tokuyama, T. Fukuyama
　　Chem. Asian J., 3, 296-309 (2008)

(70) Synthetic Studies on Haplophytine: Protective Group Controlled Rearrangement
　　K. Matsumoto, H. Tokuyama, T. Fukuyama
　　Synlett., 3137-3140 (2007)

(69) Synthesis of vinyloxazolidinones by palladium-catalyzed CO₂-recycling reaction of 4-(benzylamino)-2-butenyl carbonates
　　M. Yoshida, Y. Ohsawa, K. Sugimoto, H. Tokuyama, M. Ihara
　　Tetrahedron Lett., 48, 8678-8682 (2007)

(68) Synthesis of (+)-Vinblastine and Its Analogs
　　T. Miyazaki, S. Yokoshima, S. Shimizu, H. Osada, H. Tokuyama, T. Fukuyama
　　Org. Lett., 9, 4737-4740 (2007)

(67) Design and Synthesis of Thiazoline-Thiazole Hybrid Macrocycles Possessing Strong Binding Affinity to Pb²⁺ and Cd²⁺
　　F. S. Han, H. Tokuyama, T. Fukuyama
　　Chem. Commun., 3444-3446 (2007)

(66) Cascade and One-pot Processes Providing Substituted Quinolines from Aldimines and Allylsilanes: Auto-tandem Catalysis of Triflic Imide
　　N. Shindoh, H. Tokuyama, K. Takasu
　　Tetrahedron Lett., 48, 4749-4753 (2007)

(65) Stereocontrolled Total Synthesis of (-)-Kainic Acid
　　H. Sakaguchi, H. Tokuyama, T. Fukuyama
　　Org. Lett., 9, 1635-1638 (2007)

(64) Novel Structural Motifs Consisting of Chiral Thiazolines: Synthesis, Molecular Recognition, and Anticancer Activity
　　F. S. Han, H. Osajima, M. Cheung, H. Tokuyama, T. Fukuyama
　　Chem. Eur. J. 13, 3026-3036 (2007)

(63) A Novel Indole Synthesis via Conjugate Addition of Pyrrolidine to o-Nitrophenylacetylenes
　　H. Tokuyama, T. Makido, Y. Han-ya, T. Fukuyama
　　Heterocycles, 72, 191- 197 (2007)

(62) Catalytic Imino Diels-Alder Reaction by Triflic Imide and Its Application to One-pot Synthesis from Three Components
　　K. Takasu, N. Shindoh, H. Tokuyama, M. Ihara
　　Tetrahedron, 62, 11900-11907 (2006)

(61) Total Synthesis of (+)-Yatakemycin
　　K. Okano, H. Tokuyama, T. Fukuyama
　　J. Am. Chem. Soc., 128, 7136-7137 (2006)

(60) Synthesis of Chiral Cyclic Oligothiazolines: A Novel Structural Motif of Macrocyclic Molecule
　　F. S. Han, H. Osajima, M. Cheung, H. Tokuyama, T. Fukuyama
　　Chem. Commun., 1757-1758 (2006)

(59) Stereocontrolled Total Synthesis of (-)-Eudistomin C
　　T. Yamashita, N. Kawai, H. Tokuyama, T. Fukuyama
　　J. Am. Chem. Soc., 127, 15038-15039 (2005)

(58) Synthesis of Tetrahydro-beta -carbolines via Radical Cyclization of 2-Alkenylthioanilides
　　M. Iwadate, T. Yamashita, H. Tokuyama, T. Fukuyama
　　Heterocycles, 66, 241-249 (2005)

(57) Stereocontrolled Total Synthesis of (-)-Kainic Acid. Regio- and Stereoselective Lithiation of Pyrrolidine Ring with the (+)-Sparteine Surrogate
　　Y. Morita, H. Tokuyama, T. Fukuyama
　　Org. Lett., 7, 4337-4340 (2005)

(56) Synthesis of 2,3-Dialkylindoles from 2-Alkenylphenylisocyanides and Imines by Silyltelluride- and Tin Hydride-Mediated Sequential Radical Reactions
　　M. Kotani, S. Yamago, A. Satoh, H. Tokuyama, T. Fukuyama
　　Synlett, 1893-1896 (2005)

(55) Fluorescence enhancement by hydroperoxides based on the change in intramolecular charge transfer character of benzofurazan
　　M. Onoda, H. Tokuyama, S. Uchiyama, K. Mawatari, T. Santa, K. Kaneko, K. Imai, K. Nakagomi
　　Chem. Commun., 1848-1850 (2005)

(54) Thermal and Palladium-Catalyzed [3 + 2] Synthesis of Cyclopentadienone Acetals from Cyclopropenone Acetals and Acetylenes
　　H. Isobe, S. Sato, T. Tanaka, H. Tokuyama, E. Nakamura
　　Org. Lett., 6, 3569-3571 (2004)

(53) Stereocontrolled Total Synthesis of (+)-Vincristine
　　T. Kuboyama, S. Yokoshima, H. Tokuyama, T. Fukuyama
　　Proc. Natl. Acad. Sci. USA, 101, 11966-11970 (2004)

(52) Total Synthesis of (-)-Stychnine
　　Y. Kaburagi, H. Tokuyama, T. Fukuyama
　　J. Am. Chem. Soc., 126, 10246-10247 (2004)

(51) 4-(t-Butyldimethylsilyloxy)benzylidene Acetal: A Novel Benzylidene-type Protecting Group for 1,2-Diols
　　Y. Kaburagi, H. Osajima, K. Shimada, H. Tokuyama, T. Fukuyama
　　Tetrahedron Lett., 45, 3817-3821 (2004)

(50) Enanthioselective Total Synthesis of FR900482
　　M. Suzuki, M. Kambe, H. Tokuyama, T. Fukuyama
　　J. Org. Chem., 69, 2831-3843 (2004)

(49) New Odorless Protocols for the Synthesis of Aldehydes and Ketones from Thiol Esters
　　T. Miyazaki, Y. Han-ya, H. Tokuyama, T. Fukuyama
　　Synlett, 477-480 (2004)

(48) Synthesis of Secondary Arylamines through Copper-Mediated Intermolecular Aryl Amination
　　K. Okano, H. Tokuyama, T. Fukuyama
　　Org. Lett., 5, 4987-4990 (2003)

(47) Stereocontrolled Total Synthesis of (-)-Aspidophytine
　　S. Sumi, K. Matsumoto, H. Tokuyama, T. Fukuyama
　　Tetrahedron, 59, 8571-8587 (2003)

(46) A Novel Palladium-Catalyzed Coupling of Thiol Esters with 1-Alkynes
　 　H. Tokuyama, T. Miyazaki, S. Yokoshima, T. Fukuyama
　　Synlett, 1512-1514 (2003)

(45) Total Synthesis of Duocarmycins
　 　K. Yamada, T. Kurokawa, H. Tokuyama, T. Fukuyama
　　J. Am. Chem. Soc., 125, 6630-6631 (2003)

(44) Enantioselective Total Synthesis of Aspidophytine
　   S. Sumi, K. Matsumoto, H. Tokuyama, T. Fukuyama
　　Org. Lett., 5, 1891-1893 (2003)

(43) First Fluorescent Photoinduced Electron Transfer (PET) Reagent for Hydroperoxides
   　M. Onoda, S. Uchiyama, A. Endo, H. Tokuyama, T. Santa, K. Imai
　　Org. Lett., 5, 1459-1461 (2003)

(42) Stereoselective Formation of a beta-Lactam Fused Oxathiazepin: A Synthetic Approach to Eudistomins
　  T. Yamashita, H. Tokuyama, T. Fukuyama
　　Synlett, 738-741 (2003)

(41) Transformation of Primary Amines to N-Monoalkylhydroxylamines: N-Hydroxy-(S)-phenylethylamine Oxalate
 　  H. Tokuyama, T. Kuboyama, T. Fukuyama
　　Org. Synth., 80, 207-218 (2003)

(40) Stereocontrolled Total Synthesis of (+)-Vinblastine
　 　S. Yokoshima, T. Ueda, S. Kobayashi, A. Sato, T. Kuboyama, H. Tokuyama, T. Fukuyama
　　Pure Appl. Chem., 75, 29-38 (2003)

(39) Facile Construction of N-Hydroxybenzazocine: Enantioselective Total Synthesis of (+)-FR900482
　　M. Suzuki, M. Kambe, H. Tokuyama, T. Fukuyama
　　Angew. Chem. Int. Ed., 41, 4686-4688 (2002)

(38) A Novel Estrogen Receptor Binding Assay Method for Endocrine Disruptors using Fluorescence Polarization
   　K. Ohno, T. Santa, T. Fukushima, N. Waizumi, H. Tokuyama, M. Maeda, K. Imai
　　Anal. Chem., 74, 4391-4396 (2002)

(37) Synthesis of 2,3-Disubstituted Indoles by Radical Cyclization with Hypophosphorous Acid and Its Application to Total Synthesis of (±)-Catharanthine
　   M. T. Reding, Y. Kaburagi, H. Tokuyama, T. Fukuyama
　　Heterocycles, 56, 313-330 (2002)

(36) One-Pot Claisen Rearrangement with n-Butyl Vinyl Ether
　　H. Tokuyama, T. Makido, T. Ueda, T. Fukuyama
　　Syn. Commun., 32, 869-873 (2002)

(35) A Mild Copper-Mediated Intramolecular Amination of Aryl Halides
　　K. Yamada, T. Kubo, H. Tokuyama, T. Fukuyama
　　Synlett, 231-234 (2002)

(34) A Novel Conversion of alpha-Aminonitrile to Amide
　 　S. Yokoshima, T. Kubo, H. Tokuyama, T. Fukuyama
　　Chem. Lett., 122-124 (2002)

(33) Stereocontrolled Total Synthesis of Vinblastine
　　S. Yokoshima, T. Ueda, S. Kobayashi, A. Sato, T. Kuboyama, H. Tokuyama, T. Fukuyama
　　J. Am. Chem. Soc., 124, 2137-2139 (2002)

(32) Reduction of Ethanethiol Esters to Aldehydes
　 　H. Tokuyama, S. Yokoshima, S.-C. Lin, L. Li, T. Fukuyama
　　Synthesis, 1121-1123 (2002)

(31) A Practical Route to Quinoline from Anilines
　　H. Tokuyama, M. Sato, T. Ueda, T. Fukuyama
　　Heterocycles, 54, 105-108 (2001)

(30) 1,3-Dipolor Cycloaddition Strategy for Enatioselective Total Synthesis of FR-900482 Analogues
　　M. Kambe, E. Arai, M. Suzuki, H. Tokuyama, T. Fukuyama
　　Org. Lett., 3, 2575-2578 (2001)

(29) A Novel Protocol for Construction of Indolylmethyl Group at Aldehydes or Ketones
　　H. Tokuyama, M. Watanabe, Y. Hayashi, T. Kurokawa, G. Peng, T. Fukuyama
　　Synlett, 1403-1406 (2001)

(28) Synthesis of 2,3-Disubstituted Indoles by Palladium-Mediated Coupling of 2-Iodoindoles
　　H. Tokuyama, Y. Kaburagi, X. Chen, T. Fukuyama
　　Synthesis, 429-434 (2000)

(27) A Novel Transformation of Primary Amines to N-Monoalkylhydroxylamines
　　H. Tokuyama, T. Kuboyama, A. Amano, T. Yamashita, T. Fukuyama
　　Synthesis, 1299-1304 (2000)

(26) Enatioselective Total Synthesis of (+)-Gelsemine: Determination of Its Absolute Configuration
　　S. Yokoshima, H. Tokuyama, T. Fukuyama
　　Angew. Chem. Int. Ed., 39, 4073-4075 (2000)

(25) Radical Cyclization of 2-Alkenylthioanilides: A Novel Synthesis of 2,3-Disubstituted Indoles
　　H. Tokuyama, T. Yamashita, M. T. Reding, Y. Kaburagi, T. Fukuyama
　　J. Am. Chem. Soc., 121, 3791-3792 (1999)

(24) Cyclopropenone-Containg Cysteine Proteinase Inhibitors. Synthesis and Enzyme Inhibitory Activites
　　R. Ando, T. Sakaki, Y. Morinaka, C. Takahashi, Y. Tamao, N. Yoshii, S. Katayama, K. Saito, H. Tokuyama, M. Isaka, E. Nakamura
　　Bioorg. Med. Chem. 7, 571-579 (1999)

(23) 2-(2-Aminophenyl)-Acetoaldehyde Dimethyl Acetal: A Novel Reagent for the Protection of Carboxylic Acids
　　E. Arai, H. Tokuyama, M. S. Linsell, T. Fukuyama
　　Tetrahedron Lett., 39, 71-74 (1998)

(22) A Novel Ketone Synthesis by a Palladium-Catalyzed Reaction of Thiol Esters and Organozinc Reagents
　　H. Tokuyama, S. Yokoshima, T. Yamashita, T. Fukuyama
　　Tetrahedron Lett., 39, 3189-3192 (1998)

(21) Facile Palladium-Mediated Conversion of Ethanethiol Esters to Aldehydes and Ketones
　　H. Tokuyama, S. Yokoshima, T. Yamashita, S.-C. Lin, L. Li, T. Fukuyama
　　J. Braz. Chem. Soc., 9, 381-387 (1998)

(20) Synthetic and Computational Studies on Symmetry-Defined Double Cycloaddition of a New Tris-Annulating Reagent to C60
　　H. Isobe, H. Tokuyama, M. Sawamura, E. Nakamura
　　J. Org. Chem., 62, 5034-5041 (1997)

(19) Nitrene Additions to [60]Fullerene Do Not Generate [6,5] Aziridines
　　A. B. Smith, III, H. Tokuyama
　　Tetrahedron, 52, 5257-5262 (1996)

(18) Biological Acitvity of Water-Soluble Fullerenes. Structure Dependence of DNA Cleavage, Cytotoxicity, and Enzyme Inhibitory Activities Including HIV-Protease Inhibition
　　E. Nakamura, H. Tokuyama, S. Yamago, T. Shiraki, Y. Sugiura
　　Bull. Chem. Soc. Jpn., 69, 2143-2151 (1996)

(17) Photocytotoxicity of Water-Soluble Fullerene Derivatives
　　K. Irie, Y. Nakamura, H. Ohigashi, H. Tokuyama, S. Yamago, E. Nakamura
　　Biosci. Biotech. Biochem., 60, 1359-1361 (1996)

(16) Regio- and Diastereo-Controlled Double Cycloaddition to [60]Fullerene: One-step Synthesis of Cs and C2 Chiral Organofullerenes with New Tris Annulating Reagents
　　E. Nakamura, H. Isobe, H. Tokuyama, M. Sawamura
　　J. Chem. Soc., Chem. Commun., 1747-1748 (1996)

(15) Structure of Fullerene Anchored by Five-membered-ring
　　H. Amano, H. Uekusa, Yuji Ohashi, H. Tokuyama, E. Nakamura
　　Mol. Cryst. Liq. Cryst. 276, 291-294 (1996)

(14) Methano- and Propanofullerenes by [1+2] and [3+2] Cycloaddition of Vinylcarbene Species
　　H. Tokuyama, H. Isobe, E. Nakamura
　　Bull. Chem. Soc. Jpn., 68, 935-941 (1995)

(13) In vivo Biological Behavior of a Water-Miscible Fullerene: 14C Labeling, Absorption, Distribution, Excretion and Acute Toxicity
　　S. Yamago, H. Tokuyama, E. Nakamura, K. Kikuchi, S. Kananishi, K. Sueki, H. Nakahara, S. Enomoto, F. Ambe
　　Chem. Biol., 2, 385-389 (1995)

(12) Synthesis of Cyclopropenone-Containing Amino Acid Mimic. Addition of Cyclopropenyl Cerium Reagent to -Amino Aldehydes
　　H. Tokuyama, M. Isaka, E. Nakamura
　　Synth. Commun., 25, 2005-2012 (1995)

(11) Synthesis of Oxo- and Methylene-Bridged C60 Dimers, the First Well-Characterized Species Containing Fullerene-Fullerene Bonds
　　A. B. Smith, III, H. Tokuyama, R. M. Strongin, G. T. Furst, W. J. Romanow, B. T. Chait, U. A. Mirza, I. Haller
　　J. Am. Chem. Soc., 117, 9359-9360 (1995)

(10) Photoaddition of Silyl Ketene Acetal to [60]Fullerene. Synthesis of -Fullerene-substituted Carboxylic Esters
　　H. Tokuyama, H. Isobe, E. Nakamura
　　J. Chem. Soc., Chem. Commun., 2753-2754 (1994)

(9) Synthetic Chemistry with Fullerenes. Photooxygenation of Olefins
　　H. Tokuyama, E. Nakamura
　　J. Org. Chem., 59, 1135-1138 (1994)

(8) Fullerene-Oligonucleotide Conjudates: Photo-induced Sequence-Specific DNA Cleavage
　　A. S. Boutorine, H. Tokuyama, M. Takasugi, H. Isobe, E. Nakamura, C. Helene
　　Angew. Chem. Int. Ed. Engl., 33, 2462-2465 (1994)

(7) A New Class of Proteinase Inhibitor. Cyclopropenone-Containing Inhibitor of Papain
　　R. Ando, Y. Morinaka, H. Tokuyama, M. Isaka, E. Nakamura
　　J. Am. Chem. Soc., 115, 1174-1175 (1993)

(6) Regioselective Generation and Stereoselective [1+2] Cycloaddition of Substituted Vinylcarbenes
　　H. Tokuyama, T. Yamada, E. Nakamura
　　Synlett, 589-591 (1993)

(5) Photoinduced Biochemical Activity of Fullerene Carboxylic Acid
　　H. Tokuyama, S. Yamago, E. Nakamura, T. Shiraki Y. Sugiura
　　J. Am. Chem. Soc., 115, 7918-7919 (1993)

(4) Chemical Derivatization of Organofullerenes through Oxidation, Reduction, and C-O and C-C Bond-Forming Reactions
　　S. Yamago, H. Tokuyama, E. Nakamura, M. Prato, F. Wudl
　　J. Org. Chem., 58, 4796-4798 (1993)

(3) [1+2] and [3+2] Cycloaddition Reaction of Vinylcarbenes with C60
　　H. Tokuyama, M. Nakamura, E. Nakamura
　　Tetrahedron Lett., 34, 7429-7432 (1993)

(2) Thermal Reactions of Substituted Cyclopropenone Acetals. Regio- and Stereochemistry of Vinylcarbene Formation and Low-Temperature [3+2] Cycloaddition
　　H. Tokuyama, M. Isaka, E. Nakamura
　　J. Am. Chem. Soc., 114, 5523-5530 (1992)

(1) Synthesis and Biological Activities of Cyclopropenone Antibiotic Penitricin and Congeners
　　H. Tokuyama, M. Isaka, E. Nakamura
　　J. Antibiot., 45, 1148-1154 (1992)

Reviews and Accounts

(15) ついに合成！難攻不落のアザジラクチン
　　K. Sugimoto, H. Tokuyama
　　Kagaku (Kyoto), 62, 70-71 (2007)

(14) Total Syntheses of FR900482
　　H. Tokuyama, M. Suzuki, T. Fukuyama,
　　J. Synth. Org. Chem., Jpn, 65, 470-480 (2007)

(13) Acceleration of Reaction by Microwave Irradiation
　　H. Tokuyama, M. Nakamura
　　J. Synth. Org. Chem., Jpn, 63, 1893-1896 (2005)

(12) 「インドール合成の進展とその応用」
　　徳山英利
　　現代化学増刊４３「最新有機合成化学ーさまざまな元素の活用」、東京化学同人、２００５年

(11) Palladium-Mediated Synthesis of Aldehydes and Ketones from Thiol Esters
　　T. Fukuyama, H. Tokuyama
　　Aldrichimica Acta, 37, 87-96 (2004)

(10) 「世界をリードする日本の化学、実用的な有機合成を目指すービンブラスチン全合成の考え方ー」
　　福山　透、徳山英利
　　現代化学、２００４年７月号、pp38-43

(9) Development of New Synthetic Methods and Their Application to Synthesis of Useful Compounds
　　H. Tokuyama
　　Yakugaku Zasshi, 123, 1007-1021 (2003)

(8) Synthesis of 2,3-Disubstituted Indoles by Radical Cyclization of 2-Alkenylphenylisocyanide
　　H. Tokuyama and T. Fukuyama
　　Chem. Rec., 2, 37-45 (2002)

(7) Development and Application of A Novel Indole Synthesis and Useful Functional Group Transformations
　　H. Tokuyama and T. Fukuyama
　　有機合成　創造の軌跡　126のマイルストーン　有機合成化学協会編、2002年、pp224-225

(6) New Development of Indole Synthesis using Radical Cyclization and Application to Indole Alkaloid Synthesis
　　H. Tokuyama
　　J. Synth. Org. Chem., Jpn, 59, 488-489 (2001)

(5) Development of new indole synthesis and application to synthesis of natural products
　　H. Tokuyama, T. Fukuyama
　　Kagaku Kogyo, 52, 416-421 (2001)

(4) Total Synthesis of Antibiotic Vancomycin
　　H. Tokuyama, T. Fukuyama
　　Kagaku (Kyoto), 55, 68-69 (2000)

(3) Efficient Synthesis of Nitrogen-Containing Natural Products
　　H. Tokuyama, T. Fukuyama
　　Farumashia, 34, 1208-1212 (1998)

(2) Pharmacokinetic and Toxicity Studies on Water-Miscible Fullerenes
　　E. Nakamura, S. Yamago, H. Tokuyama, K. Kuchi, S. Kananishi, K. Sueki, H. Nakahara, S. Enomoto, and F. Ambe
　　"New Horizons in Organic Synthesis, V. Nair and S. Jumar, Eds., New Age International, New Delhi, 1997, pp. 207-212

(1) Synthesis of Organic Derivatives of Fullerenes
　　S. Yamago, H. Tokuyama, E. Nakamura, M. Prato, and F. Wudl
　　Trans. Mat. Res. Soc. Jpn, 14B, 1169-1172 (1994)

(5) 「大学院講義有機化学演習編」分担執筆、野依良治ら編、東京化学同人、2007

(4) 「天然物化学ー植物編」分担執筆、山村庄亮、長谷川宏司編、アイピーシー、2007　

(3) 「演習で学ぶ　有機反応機構」共著、共編、有機合成化学協会編、化学同人、2005

(2) 「化学系薬学　I. 化学物質の性質と反応」分担執筆、日本薬学会編、東京化学同人、2004

(1) 「有機合成　創造の軌跡　126のマイルストーン」共編、有機合成化学協会編、化学同人、2002