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トップページ >  English >  CV >  Professor Toshiyuki KAN, Ph.D

Professor Toshiyuki KAN, Ph.D


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Toshiyuki Kan, Ph.D.
Professor


Personal Information:

Date of birth: February 15, 1964

Married: Maki Kan

Children: Natsuki Kan

School of Pharmaceutical Sciences University of Shizuoka University
52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan

Phone : 81-54-264-5746 FAX : 81-(0)-54-264-5745
e-mail : kant@u-shizuoka-ken.ac.jp
Home Page : https://www.us-yakuzo.jp/english/index.html

Education

B.S., Chemistry, March, 1986. Hokkido University, Sapporo, Hokkaido.
Under Professor Takeshi Matsumoto on "Synthetic Study of Thrsiferyl-23-acetate".
M.S., Chemistry, March, 1988. Hokkido University, Sapporo, Hokkaido.
Under Professor Haruhisa Shirahama on "Total Synthesis of Thrsiferyl-23-acetate".
Ph.D.,Chemistry, March, 1993. Hokkido University, Sapporo, Hokkaido.
Under Professor Haruhisa Shirahama on "Total Synthesis of Grayanotoxin III".

Honors and Awards

Incentive Award, The Society of Synthetic Organic Chemistry, Japan (2002)
Research Vision Division Award, 2003, Pharmaceutical Society of Japan (2004)
Pfizer Distinguished Lecture, Colorado State University (2012)
Asteras Life Science Award, The Society of Synthetic Organic Chemistry, Japan (2012)

Research and Professional Experience

Professor, University of Shizuoka, April 2004 ~ present.
Associate Professor, Tokyo University, November 2003 ~ March 2004.
Assistant Professor, Tokyo University, April 1996~October 2003.
Researcher, Suntory Institute for Bioorganic Research, June 1993 ~ March 1996.

Professional Society Memberships

American Chemical Society
Chemical Society of Japan
Society of Synthetic Organic Chemistry in Japan
Pharmaceutical Society of Japan

Publications

(138) Synthesis of chemical-biology tools enabling vivo imaging and analysis of epigallocatechin gallate
Tomohiro Asakawa, Atsushi Yoshida, Yasuo Hirooka, Takashi Suzuki, Kunihiko Itoh, Kosuke Shimizu, Naoto Oku, Takumi Furuta,Toshiyuki Wakimoto, Makoto Inai, Toshiyuki Kan
CABI (2017) in press.

(137)N-Glucosides of Fairy Chemicals, 2-Azahypoxanthine and 2-Aza-8-oxohypoxanthine, in Rice
Choi, Jae-Hoon, Wu, Jing, Sawada, Azusa, Takeda, Syougo, Takemura, Hirohide, Yogosawa, Kaoru ; Hirai, h; Kondo Mitsuru, Sugimoto Kunihisa, Asakawa Tomohiro, Inai Makoto, Kan Toshiyuki, Kawagishi Hirokazu.
Org. Lett., 20(1), 312-314 (2018).

(136) Rapid LC-MS Determination of Acromelic Acids A and B, Toxic Constituents of the Mushroom Paralepistopsis acromelalga
Naoki Yoshioka, Hitoshi Ouchi, Toshiyuki Kan, Masashi Yoshida, Motoyuki Nomura
Food Hygiene and Safety Science 58, 241-245 (2017).

(135)Total Synthesis of TAN1251C via Diastereoselective Construction of the Azaspiro Skeleton
Yosuke Nagasaka, Sayaka Shintaku, Kosuke Matsumura, Akitaka Masuda, Tomohiro Asakawa, Makoto Inai, Masahiro Egi, Yoshitaka Hamashima, Yoshinobu Ishikawa, Toshiyuki Kan
Org. Lett., 19, 3832-3842 (2017) .

(134) Synthetic Study on Pactamycin: Stereoselective Synthesis of the Cyclopentane Core Framework
Atsumi Goto, Satoshi Yoshimura, Yuta Nakao, Makoto Inai, Tomohiro Asakawa, Masahiro Egi, Yoshitaka Hamashima, Mitsuru Kondo and Toshiyuki Kan
Org. Lett., 19, 3358-3361 (2017).

(133) Efficient synthesis of 3-amino-1,5-benzodiazepine-2-one derivatives
Nobuhiro Obara,Takeshi Watanabe, Tomohiro Asakawa, Toshiyuki Kan, Takao Tanakaa
Synlett, 28, 1183-1186 (2017)

(132) Divergent synthesis of kinase inhibitor derivatives, leading to discovery of selective Gck inhibitors
Takanori Matsumaru, Makoto Inai, Kana Ishigami, Toshiki Iwamatsu, Hiroshi Maita, Satoko Otsuguro, Takao Nomura, Akira Matsuda, Satoshi Ichikawa, Masahiro Sakaitani, Satoshi Shuto, Katsumi Maenaka and Toshiyuki Kan
Bioorg. Med. Chem. Lett. 27, 2144-2147 (2017).

(131) Insulinotropic and anti-apoptotic effects of nobiletin in INS-1D ß-cells Insulinotropic and anti-apoptotic effects of nobiletin in INS-1D ß-cells
Miki Takii, Yukiko K. Kaneko, Kiriko Akiyama, Yuki Aoyagi, Yuki Tara, Tomohiro Asakawa, Makoto Inai, Toshiyuki Kan, Kiyomitsu Nemoto, Tomohisa Ishikawa
J. Funct. Foods, 30, 8-15 (2017).

(130) Synthesis of chemical-biology tools enabling vivo imaging and analysis of epigallocatechin gallate.,
Tomohiro Asakawa, Atsushi Yoshida, Yasuo Hirooka, Takashi Suzuki, Kunihiko Itoh, Kosuke Shimizu, Naoto Oku, Takumi Furuta,Toshiyuki Wakimoto,Makoto Inai, and Toshiyuki Kan
Heterocycles, 93, 218-242 (2016).

(129) Stereoselective Construction of 2-Vinyl 3-Hydroxybenzopyran Rings: Total Syntheses of Teadenols A and B.
Ryunosuke Yoshida, Hitoshi Ouchi, Tomohiro Asakawa, Makoto Inai, Masahiro Egi, Yoshitaka Hamashima, Toshiyuki Kan
Org. Biomol. Chem., 14, 10783-10786 (2016).

(127) Concise synthesis of anserine: efficient solvent tuning in asymmetric hydrogenation reaction
Megumi Yamashita, Keita Shimizu, Yasuaki Koizumi, Toshiyuki Wakimotoa, Yoshitaka Hamashima, Tomohiro Asakawa, Makoto Inai, Toshiyuki Kan
Synlett, 27, 2734-2736 (2016)

(126) Practical synthesis of spermine, thermospermine and norspermine
Yuka Kariya, Yuta Asanuma, Makoto Inai, Tomohiro Asakawa, Kyoko Ohashi-Ito, Hiroo Fukuda, Masahiro Egi, Toshiyuki Kan
Chem. Pharm. Bull., 64, 1403-1407 (2016)

(125) Applications of C-H Insertion Reaction in Total Synthesis of Biologically Active Heterocyclic Natural Products
Toshiyuki Kan, Tomohiro Asakawa, and Makoto Inai
Heterocycles, 92, 31-43 (2016)

(124) Syntheses of methylated catechins and theaflavins using the Ns group to protect and deactivate the phenol
Tomohiro Asakawa, Yusuke Kawabe, Atsushi Yoshida, Yoshiyuki Aihara, Tamiko Manabe, Yoshitsugu Hirose, Asuka Sakurada, Makoto Inai, Yoshitaka Hamashima, Takumi Furuta, Toshiyuki Wakimoto, Toshiyuki Kan
J. Antibiot., 69, 299-312 (2016)

(123) Synthesis of food effective constituents toward the development for chemical biology investigations.
Makoto Inai, Tomohiro Asakawa Toshiyuki Kan
J. Syn. Org. Chem., Jpn, 74, 412 (2016).

(122) Synthesis of Food Effective Constituents toward the Development for Chemical Biology Investigations
Makoto Inai, Tomohiro Asakawa Toshiyuki Kan
J. Syn. Org. Chem., Jpn, in press.

(121) Synthesis of Chemical-Biology Tools Enabling Vivo Imaging and Analysis of Epigallocatechin Gallate
T. Asakawa, A. Yoshida, Y. Hirooka, T. Suzuki, K. Itoh, K. Shimizu, N. Oku, T. Furuta,T. Wakimoto, M.Inai, T. Kan
Heterocycles, in press.

(120) A Negative Feedback Loop Controlling bHLH Complexes is Involved in Vascular Cell Division and Differentiation in the Root Apical Meristem
H. Katayama, K. Iwamoto, Y. Kariya, T. Asakawa, T. Kan, H. Fukuda, K. Ohashi-Ito
Current Biology, 25, 3144-3150 (2015).

(119) Stereocontrolled Total Syntheses of Optically Active Furofuran Lignans
Inai, M.; Ishikawa, R.; Yoshida, N.; Shirakawa, N.; Akao, Y.; Kawabe, Y.; Asakawa, T.; Egi, M.; Hamashima, Y.; Kan, T.
Synthesis, 47, 3413-3521 (2015).

(118) Ecteinascidins. A review of the chemistry, biology and clinical utility of potent tetrahydroisoquinoline antitumor antibiotic
V. H. Le, M. Inai, R. M. Williams and T. Kan
Natural Product Reports, 32, 328-347 (2015).

(117)The “fairy” (2-azahypoxanthine) produced by the fairy-ring-forming fungus promotes the growth and the grain yield of rice
Asai, T., Choi, J-H., Ikka, T., Fushimi, K., Abe, N., Tanaka, H., Yamakawa, Y., Kobori, H., Kiriiwa, Y., Motohashi, R., Deo, V. P., Asakawa, T., Kan, T., Morita, A. and Kawagishi, H., Jpn.
Agric. Res. Quart, 49, 45-49 (2015).

(116) Total Syntheses of (+)-Sesamin and (+)-Sesaminol.
Ryo Ishikawa, Naoto Yoshida, Yusuke Akao, Yusuke Kawabe, Makoto Inai, Tomohiro Asakawa, Yoshitaka Hamashima, and Toshiyuki Kan
Chemistry Letters, 43, 1572-1574 (2014). Editor’s Choice

(115) 3, 3', 4', 5'-tetrahydroxyflavone induces formation of large aggregates of amyloid β protein.
H. Ushikubo, Y. Tanimoto, K. Abe, T. Asakawa, T. Kan and T. Akaishi
Biol. Pharm. Bull., 37, 748–754 (2014).

(114) Practical Synthesis of plant-growth regulators; AHX, AHXR and AOH, and development of their probe molecules
Kazutada Ikeuchi, Ryosuke Fujii, Shimpei Sugiyama, Tomohiro Asakawa, Makoto Inai, Yoshitaka Hamashima, Jae-Hoon Choi, Tomohiro Suzuki, Hirokazu Kawagishi, and Toshiyuki Kan
Organic & Biomolecular Chemistry, 12, 3813-3815 (2014).

(113) Synthesis of biological active natural products by means of C-H insertion reaction,
Toshiyuki Kan
J. Syn. Org. Chem., Jpn, 72, 171 (2014).

(112) Neuroprotective effect of nobiletin on cerebral ischemia?reperfusion injury in transient middle cerebral artery-occluded rats:
Nodoka Yasuda, Takayuki Ishii, Dai Oyama, Tatsuya Fukuta, Yurika Agato, Akihiko Sato, Kosuke Shimizu, Tomohiro Asai, Tomohiro Asakawa, Toshiyuki Kan, Shizuo Yamada, Yasushi Ohizumi, Naoto Oku
Brain Res.,1559, 46-54 (2014).

(111) 2-Azahypoxanthine and imidazole-4-carboxamide produced by the fairy-ring-forming fungus increases wheat yield Field Crops Research
Field Crops Res., 162C, 1-6 (2014).

(110) Practical Total Synthesis of Acromelic acid A and B
Hitoshi Ouchi, Aya Asahina, Tomohiro Asakawa, Makoto Inai, Yoshitaka Hamashima and Toshiyuki Kan.
Org. Lett., 16, 1980-1983 (2014).

(109) Stereocontrolled Total Synthesis of Hedyotol A
Yusuke Kawabe, Ryo Ishikawa, Yusuke Akao, Atsushi Yoshida, Makoto Inai, Tomohiro Asakawa, Yoshitaka Hamashima, Toshiyuki Kan
Org. Lett., 16, 1976-1979 (2014).

(108) Total Synthesis of (-)-SB-203207
Yasuo Hirooka, Kazutada Ikeuchi, Yuichiro Kawamoto, Yusuke Akao, Takumi Furuta, Tomohiro Asakawa, Makoto Inai, Toshiyuki Wakimoto, Tohru Fukuyama, and Toshiyuki Kan
Org. Lett., 16, 1646-1649 (2014).

(107) The Source of "Fairy Rings": 2-Azahypoxanthine and its Metabolite Found in a Novel Purine Metabolic Pathway in Plants
Jae-Hoon Choi, Toshiyuki Ohnishi, Yasuhiro Yamakawa, Shogo Takeda, Shuhei Sekiguchi, Waki Maruyama, Kimiko Yamashita, Tomohiro Suzuki, Akio Morita, Takashi Ikka, Reiko Motohashi, Yoshikazu Kiriiwa, Hiroyuki Tobina, Tatsuo Asai, Shinji Tokuyama, Hirofumi Hirai, Nobuhiro Yasuda, Keiichi Noguchi, Tomohiro Asakawa, Shimpei Sugiyama, Toshiyuki Kan, and Hirokazu Kawagishi
Angew. Chem. Int. Ed., 53, 1552-1555 (2014).

(106) Use of positron emission tomography for real-time imaging of biodistribution of green tea catechin
Kosuke Shimizu, Tomohiro Asakawa, Norihiro Harada, Dai Fukumoto, Hideo Tsukada, Tomohiro Asai, Shizuo Yamada, Toshiyuki Kan, and Naoto Oku
PLOS ONE, e85520 (2014).

(105) Practical Synthesis of Kainoids and its Application to the Probe Molecules
Shingo Sasaki, Hiroto Suzuki, Hitoshi Ouchi, Tomohiro Asakawa, Makoto Inai, Yoshitaka Hamashima, Ryuichi Sakai, Keiko Shimamoto, and Toshiyuki Kan.
Org. Lett., 16, 564-567 (2014).

(104) Synthetic Studies of Fisetin, Myricetin and Nobiletin Analogs and Related Probe Molecules
Aiki Hiza, Yuta Tsukaguchi, Takahiro Ogawa, Makoto Inai, Tomohiro Asakawa, Yoshitaka Hamashima, and Toshiyuki Kan
Heterocycles, 88, 1371-1396 (2014).

(103) Stereocontrolled Total Synthesis of Sphingofungin E
Kazutada Ikeuchi, Moemi Hayashi, Tomohiro Yamamoto, Makoto Inai, Tomohiro Asakawa, Yoshitaka Hamashima, and Toshiyuki Kan.
Eur. J. Org. Chem., 6789 (2013).

(102) Chemical Synthesis of Tea Polyphenols and Related Compounds
Tomohiro Asakawa, Yoshitaka Hamashima, Toshiyuki Kan
Current Pharmaceutical Design, 19, 6207 (2013)

(101) Effects of green tea catechins on cytochrome P450 2B6, 2C8, 2C19, 2D6 and 3A Activities in Human Liver and Intestinal Microsomes
Misaka, Shingen; Kawabe, Keisuke; Onoue, Satomi; Werba, Jose Pablo; Giroli, Monica; Tamaki, Sekihiro; Kan, Toshiyuki; Kimura, Junko; Watanabe, Hiroshi; Yamada, Shizuo
Drug Metabolism and Pharmacokinetics, 28, 244-249 (2013).

(100) Physicochemical and Biopharmaceutical Characterization of Amorphous Solid Dispersion of Nobiletin, a Citrus Polymethoxylated Flavone, with Improved Hepatoprotective Effects
Satomi Onoue, Tatsuya Nakamura, Atsushi Uchida, Kazunori Ogawa, Kayo Yuminoki, Naofumi Hashimoto, Aiki Hiza, Yuta Tsukaguchi, Tomohiro Asakawa, Toshiyuki Kan, Shizuo Yamada
Euro. J. Pharm. Sci., 49, 453-460 (2013).

(98) Chemoselective Hydrogenation Reaction of Unsaturated Bonds in the Presence of o-Nitrobenzenesulfonyl Group
Akinori Kawanishi, Chiyako Miyamoto, Yuki Yabe, Makoto Inai, Tomohiro Asakawa, Yoshitaka Hamashima, Hironao Sajiki, Toshiyuki Kan
Org. Lett., 15, 1306-1309 (2013).

(97)Stereocontrolled Total Synthesis of (-)-FR901483
Shigeru Ieda, Akitaka Masuda, Mami Kariyama, Toshiyuki Wakimoto, Tomohiro Asakawa, Tohru Fukuyama,Toshiyuki Kan
Heterocycles, 86, 1071-1092 (2012).

(96) Catalytic Desymmetrization of Cyclohexadienes by Asymmetric Bromolactonization
Kazutada Ikeuchi, Shunsuke Ido, Satoshi Yoshimura, Tomohiro Asakawa, Makoto Inai, Yoshitaka Hamashima, andToshiyuki Kan
Org. Lett., 14, 6016-6019 (2012).

(95) Analysis of Nε-ethyllysine in human plasma proteins by gas chromatography-negative ion chemical ionization/mass spectrometry as a biomarker for exposure to acetaldehyde and alcohol
Ryota Mabuchi, Aya Kurita, Noriyuki Miyoshi, Akira Yokoyama, Takumi Furuta, Toshinao Goda, Yoshihide Suwa, Toshiyuki Kan, Takashi Amagai, Hiroshi Ohshima
Alcoholism: Clinical & Experimental Research, 36, 1013-1020 (2012).

(94) Stereocontrolled Total Synthesis of (+)-UCS1025A
Kenji Uchida, Takahiro Ogawa, Yoshinori Yasuda, Hiraku Mimura, Teppei Fujimoto, Tohru Fukuyama, Toshiyuki Wakimoto, Tomohiro Asakawa, Yoshitaka Hamashima and Toshiyuki Kan
Angew. Chem. Int. Ed., 51, 12850-12853 (2012) .

(93) Total Synthesis of (-)-Lemonomycin
Atsushi Yoshida, Michinori Akaiwa, Yoshitaka Hamashima, Satoshi Yokoshima, Tohru Fukuyama and Toshiyuki Kan
Chem. Eur. J., 18, 11192-11195 (2012).

(92) A Short-step Asymmetric Synthesis of Dehydrodiconiferyl Alcohol by Means of C-H Insertion Reaction Shogo Matsumoto, Tomohiro Asakawa, Yoshitaka Hamashima, and Toshiyuki Kan
Synlett, 1082-1084 (2012).

(91) 3, 3’, 4’, 5, 5’-pentahydroxyflavone is a potent inhibitor of fibril formation of amyloid b protein
Hiroko Ushikubo, Sayaka Watanabe, Yui Tanimoto, Kazuho Abe, Aiki Hiza, Takahiro Ogawa, Tomohiro Asakawa, Toshiyuki Kan, Tatsuhiro Akaishi
Neuroscience Letters, 513(1), 51-56 (2012).

(90) Furan fatty acid as an anti-inflammatory component from green-lipped mussel, Perna canaliculus. T. Wakimoto, H. Kondo, H, Nii, K. Kimura, Y. Egami, Y. Oka, M. Yoshida, E. Kida, Y. Ye, S. Akahoshi, T. Asakawa, K. Matsumura, H. Ishida, H. Nukaya, K. Tsuji, T. Kan, I. Abe
Proc. Natl. Acad. Sci. USA, 108, 17533-17537 (2011).

(89) Enantioselective Total Synthesis of Aperidine
Toshiyuki Wakimoto, Kakeru Miyata, Hitoshi Ouchi, Tomohiro Asakawa, Haruo Nukaya, Yoshihide Suwa, Toshiyuki Kan
Org. Lett., 13, 2789-2791 (2011).

(88) Stereocntrolled Synthesis of (+)-Methoxyphenylkainic acid and (+)-Phenylkainic acid
Takumi Higashi, Yoichiro Isobe, Hitoshi Ouchi, Hiroto Suzuki, Yuko Okazaki, Tomohiro Asakawa, Takumi Furuta, Toshiyuki Wakimoto, Toshiyuki Kan
Org. Lett., 13, 1089-1091 (2011).

(87) PET Imaging Investigation of Nobiletin Based on a Practical Total Synthesis
Tomohiro Asakawa, Aiki Hiza, Miho Nakayama, Makoto Inai, Dai Oyama, Hiroyuki Koide, Kosuke Shimizu, Toshiyuki Wakimoto, Norihiro Harada, Hideo Tsukada, Naoto Oku, Toshiyuki Kan*
Biol. Pharm. Bull., 34, 396-400 (2011)

(86) Anti-angiogenic activity and intracellular distribution of epigallalocatechin-3-gallate analogs
Suratsawadee PIYAVIRIYAKUL, Kosuke Shimizu, Tomohiro Asakawa, Toshiyuki Kan,
Pongun SIRIPONG, and Naoto Oku
Biol. Pharm. Bull., 34, 396-400 (2011).

(85) Proof of the existence of an unstable amino acid, pleurocybellaziridine, in Pleurocybella porrigens (angel’s wing mushroom)
Toshiyuki Wakimoto, Tomohiro Asakawa, Saeko Akahoshi, Tomohiro Suzuki, Kaoru Nagai, Hirokazu Kawagishi, Toshiyuki Kan
Angew. Chem. Int. Ed., 50, 1168-1170 (2011).

(84) Concise synthesis of catechin probes enabling analysis and imaging of EGCg
Atsushi Yoshida, Yasuo Hirooka, Yusuke Sugata, Mariko Nitta, Tamiko Manabe, Shunsuke Ido, Kouki Murakami, Repon Kumer Saha, Takashi Suzuki, Motohiro Ohshima, Akira Yoshida, Kunihiko Itoh, Kosuke Shimizu, Naoto Oku, Takumi Furuta, Tomohiro Asakawa, Toshiyuki Wakimoto, and Toshiyuki Kan
Chem. Commun., 47, 1794-1796 (2011).

(83) Diblock Copolymer of Bacterial Cellulose and Poly(methyl methacrylate) Initiated by Chain-End-Type Radicals Produced by Mechanical Scission of Glycosidic Linkages of Bacterial Cellulose.
Sakaguchi, Masato; Ohura, Takeshi; Iwata, Tadahisa; Takahashi, Shuhei; Akai, Shuji; Kan, Toshiyuki; Murai, Hisao; Fujiwara, Motoyasu; Watanabe, Osamu; Narita, Mamiko.
Biomacromolecules ACS, 11, 3059-3066 (2010).

(82) Synthesis of Axially Chiral Amino Acid
Furuta Takumi, Yamamoto Junya, Kitamura Yuki, Hashimoto Ayano, Masu Hyuma, Azumaya Isao, Kan Toshiyuki, Kawabata Takeoa
J. Org. Chem., 75. 7010-7013 (2010).

(81) Structural characteristics of green tea catechins for formation of protein carbonyl in human serum albumin
Takeshi Ishii, Taiki Mori, Tatsuya Ichikawa, Maiko Kaku, Koji Kusaka, Yoshinori Uekusa, Mitsugu Akagawa, Yoshiyuki Aihara, Takumi Furuta, Toshiyuki Wakimoto, Toshiyuki Kan, and Tsutomu Nakayama
Bioorg. Med. Chem. Lett.,18. 4892-4896 (2010).

(80) Synthesis of the Optically Active Key Intermediate of FR901483
S. Ieda, T. Kan,T. Fukuyama
Tetrahedron Letters., 51. 4027-4029 (2010).

(79) Reaction Behavior of Cumulene: Diels-Alder, Friedel-Crafts, and Pd-Catalyzed Domino Reactions
T. Asakawa, M. Iinuma, Y. Wakasugi, M. Kuno, T. Furuta, S. Fujii, K. Tanaka, T. Kan
Heterocycles, 80. 1125-1147 (2010).

(78) Binding affinity of tea catechins for human serum albumin: Characterization by high-performance affinity chromatography with immobilized albumin column.
T. Ishii, K. Minoda, M.-J. Bae, T. Mori, Y. Uekusa, T. Ichikawa, Y. Aihara, T. Furuta, T. Wakimoto, T. Kan, T. Nakayama
Molecular Nutrition and Food Research, 54, 816-822 (2010).

(77) Modified Julia-Kocienski Reaction Promoted by Means of m-NPT (Nitrophenyltetrazole) sulfone
Yuki Sakai, Kazutada Ikeuchi, Yuji Yamada, Toshiyuki Wakimoto, Toshiyuki Kan*
Synlett, 827-827 (2010).

(76) Development of Photoaffinity Probes for g-Secretase Equipped with a Nitrobenzenesulfonamide-type Cleavable Linker
S. Yokoshima, Y. Abe, N. Watanabe, Y. Kita, T. Kan, T. Iwatsubo, T. Tomita, T. Fukuyama
Bioorg. Med. Chem. Lett., 19, 6869-6871 (2009).

(75) Solid Support Synthesis of Artificial Phospholipids
T. Furuta, H. Onuki, M. Mochizuki, M. Ito, M. Inai, T.i Wakimoto, T. Kan
Synlett, 3373-3377, (2009).

(74) Structure-activity relationship study on a 1 adrenergic receptor antagonists from beer.
T.i Wakimoto, M. Nitta, K. Kasahara, T. Chiba, Y. Ye, K. Tsuji, T. Kan, H. Nukaya, M. Ishiguro, M. Koike, Y. Yokoo, Y. Suwa,
Bioorg. Med. Chem. Lett., 19, 5905-5908 (2009)

(73) Regioselective Synthesis of Methylated Epigallocatechin Gallate via Nitrobenzenesulfonyl (Ns) Protecting Group.
Y. Aihara, A. Yoshida, T. Furuta, T. Wakimoto, T. Akizawa, M. Konishi, T. Kan
Bioorg. Med. Chem. Lett., 19, 4171-4174 (2009)

(72) Stereocontrolled Total Synthesis of (±)-FR901483
S. Ieda, Y. Asoh, T. Fujimoto, H. Kitaoka, T. Kan, T. Fukuyama
Heterocycles, 79, 721-738 (2009).

(71) Concise Synthesis of Chafurosides A and B
T. Furuta, M. Nakayama, H. Suzuki, H. Tajimi, M. Inai, H. Nukaya, T. Wakimoto, T. Kan
Org. Lett., 11. 2233-2236 (2009).

(70) Identification and characterization of flavonoids as sialyltransferase inhibitors
K. I.P.J. Hidari, K. Oyama, G. Ito, M. Nakayama, M. Inai, S. Goto, Y. Kanai, K. Watanabe, K. Yoshida, T. Furuta, T. Kan, T. Suzuki
Biochemical and Biophysical Research Communications, 609-613 (2009).

(69) Total Synthesis of (±)-Morphine.
Kenji Uchida, Satoshi Yokoshima, Toshiyuki Kan, and Tohru Fukuyama,
Heterocycles, 77, 1219-1234 (2009)

(68) Stereocontrolled Total Synthesis of (?)-Myriocin
M. Inai, T. Goto, T. Furuta, T. Wakimoto, T. Kan
Tetrahedron:Asymmetry, 19, 27771-27773 (2008).

(67) Total Synthesis of (?)-Serotobenine
Y. Koizumi, H. Kobayashi, T. Wakimoto, T. Furuta, T. Fukuyama, T. Kan
J. Am. Chem. Soc., 130, 16854-16855 (2008).

(66) Efficient Synthesis of Optically Active Gallocatechin-3-gallate Derivatives via 6-endo Cyclization.
Yasuo Hirooka, Mariko Nitta, Takumi Furuta, Toshiyuki Kan
Synlett, 3234-3237 (2008).

(65) Versatile Synthesis of Head Group Functionalized Phospholipids via Oxime Bond Formation
Takumi Furuta, Masayoshi Mochizuki, Mai Ito, Tadanobu Takahashi, Takashi Suzuki, and Toshiyuki Kan
Org. Lett., 10, 4847-4850 (2008).

(64) Tackling Alzheimer’s disease by means of original synthetic methodologies in organic chemistry.
T. Kan, T. Fukuyama
J. Syn. Org. Chem., Jpn, 66, 765-773 (2008).

(63) Synthetic Studies on (+)-Manzamine A: Stereoselective Synthesis of the Tetracyclic Core Framework
Y. Kita, T. Toma, T. Kan, T. Fukuyama
Org. Lett., 10, 3251-3253 (2008).

(62) Synthesis and characteristic stereostructure of biphenanthryl ether.
Y. Koizumi, S. Suzuki, K. Takeda, K. Murahashi, M. Horikawa, K. Katagiri, H. Masu, I. Azumaya, S. Fujii, T. Furuta, K. Tanaka, T. Kan
Tetrahedron: Asymmetry, 19, 1407-1410 (2008)

(61) Synthesis of diazirine possessing an acetophenone derivative as a valuable intermediate for a flavonoid photoaffinity probe.,
T. Furuta, M. Ueda, Y. Hirooka, K. Tanaka, T. Kan,
Heterocycles, 76, 811-817 (2008).

(60) One-pot Synthesis of Carbazole via Tandem Suzuki-Miyaura and Amination Reaction
Y. Kitamura, S. Yoshikawa, T. Furuta, T. Kan
Synlett, 377-380 (2008).

(59) Synthetic Studies on Altemicidin: Stereocontrolled Construction of the Core Framework
T. Kan, Y. Kawamoto, T. Asakawa, T. Furuta, T. Fukuyama.
Org. Lett., 10, 169-171(2008).

(58) Copper-catalyzed enantioselective conjugate addition of diethylzinc using axially chiral aminoethyloxy-phosphine ligands.
T. Morimoto, N. Obara, I. Yoshida, K. Tanaka, T. Kan.
Tetrahedron Lett., 48, 3093-3095, (2007).

(57) A Versatile Synthesis of a-Amino Acid Derivatives via The Ugi Four-Component Condensation with a Novel Convertible Isonitrile.
K. Rikimaru, A. Yanagisawa, T. Kan, T. Fukuyama
Heterocycles, 73, 403-417 (2007).

(56) Divergent Synthesis of Multifunctional Molecular Probes Enabled Elucidation of the Enzyme Specificity of Dipeptidi g-Secretase Inhibitors on Presenilin-Type Aspartic Proteases
H. Fuwa, Y. Takahashi, Y. Konno, N. Watanabe, H. Miyashita, M. Sasaki, H. Natsugari, T. Kan, T. Fukuyama, T. Tomita, and T. Iwatsubo
ACS Chemical Biology, 2, 408-418 (2007).

(55) Convenient Synthesis of Photoaffinity Probes and Evaluation of Their Cross-linking Abilities.
T. Kan, Y. Kita, Y. Morohashi, Y. Tominari, S. Hosoda, H. Natsugari, T. Tomita, T. Iwatsubo and T. Fukuyama.
Org. Lett., 9, 2055-2058 (2007).

(54) Concise synthesis of dideoxy-epigallocatechin gallate (DO-EGCG) and evaluation of its anti-influenza virus activities.
T. Furuta, Y. Hirooka, A. Abe, Y. Sugata, M. Ueda, K. Murakami, T. Suzuki, K. Tanaka and T. Kan
Bioorg. Med. Chem. Lett., 17, 3095-3098 (2007).

(53) Efficient Synthesis of Phenanthridinone Derivatives via a Domino Coupling Process.
T. Furuta, Y. Kitamura, A. Hashimoto, S. Fujii, K. Tanaka and T. Kan
Org. Lett., 9, 183-186 (2007).

(52) Total Synthesis of (+)-Morphine.
K. Uchida, S. Yokoshima, T. Kan, T. Fukuyama.
Org. Lett., 8, 5311-5313 (2006).

(51) Domino Heck-C-H- Activaeion Reaction of Unsymmetrically Substitute[3]Cumulene.
T. Furuta, T. Asakawa, M. Iinuma, S. Fujii, K. Tanaka, T. Kan.
Chem. Commun., 3648-3650 (2006).

(50) Synthesis of Bicyclo[3.3.0]octane Ring System via Desymmetric C-H Insertion Reaction
T. Kan, T. Inoue, Y. Kawamoto, M. Yonehara, T. Fukuyama.
Synlett, 1583-1585 (2006)

(49) Synthesis of Biotinylated Photoaffinity Probes Based on Arylsulfonamide γ-secretase Inhibitors.
H. Fuwa, K. Hiromoto, Y. Takahashi, S. Yokoshima, T. Kan, T. Fukuyama, T. Iwatsubo, T. Tomita, H. Natsugari.
BBioorg. Med. Chem. Lett., 16, 4184-4189 (2006).

(48) Novel γ-secretase inhibitors discovered by screening in-house natural product synthesis intermediates library
Y. Takahashi, H. Fuwa, A. Kaneko, M. Sasaki, S. Yokoshima, H. Koizumi, T. Takebe, T. Kan, T. Iwatsubo, T. Tomita, H. Natsugari, T. Fukuyama.
Bioorg. Med. Chem. Lett., 16, 3813-3816 (2006).

(47) Reaction behavior of cumulene on Diels-Alder and Friedel-Crafts reaction
T. Asakawa, M. Iinuma, T. Furuta, S. Fujii, T. Kan, K. Tanaka.
Chem. Lett., 512-513 (2006).

(46) Carboxy-terminal fragment of Presenilin 1 is the molecular target of a dipeptidic g-secretase-specific inhibitor DAPT
Y. Morohashi, T. Kan, Y. Tominari, H. Fuwa, Y. Okamura, N. Watanabe, H. Natsugari, T. Fukuyama, T. Iwatsubo, T. Tomita.
J. Biol. Chem., 281, 14670-14676 (2006).

(45) Synthesis of novel phenylnaphthyl phosphines and their applications to Pd-catalyzed amidation
Y. Kitamura, A. Hashimoto, S. Yoshikawa, J. Odaira, T. Furuta, T. Kan, K. Tanaka.
Synlett, 115-117 (2006).

(44) Synthetic Studies on (-)-Lemonomycin: Stereocontrolled Construction of the 3,8-Diazabicyclo[3.2.1] Skeleton.
K. Rikimaru, K. Mori, T. Kan and T. Fukuyama.
Chem. Commun, 394-396 (2005).

(43) Acetoxy Group Directed Cyclization Promoted by SmI2: Directing Group Determined Stereocomplementarity.
T. Kan, S. Hosokawa, S. Nara, H. Tamiya, H. Shirahama, F. Matsuda.
J. Org. Chem., 69, (2004) 8956-8958.

(42) Total Synthesis of (-)-Ephedradine A (Orantine): An Efficient Construction of Optically Active Dihydrobenzofuran-ring via C-H Insertion Reaction.
W. Kurosawa, H. Kobayashi, T. Kan and Tohru Fukuyama,
Tetrahedron, 60, 9615-9628 (2004).

(41) Synthetic Studies on (+)-Naphthyridinomycin: Stereoselective Synthesis of the Tetracyclic Core Framework.
K. Mori, K. Rikimaru, T. Kan and T. Fukuyama.
Org. Lett., 6, 3095-3097 (2004).

(40) Stereocontrolled Total Synthesis of Potent Immunosuppressant FR901483.
T. Kan, T. Fujimoto, Y. Asoh, S. Ieda, H. Kitaoka and T. Fukuyama.
Org. Lett., 6, 2729-2731 (2004).

(39) Stereoselective Nucleophilic Addition Reaction with a New Chiral Template and Its Application to Synthesis of Optically Active a-Arylglycine Derivatives.
S. Tohma, K. Rikimaru, A. Endo, T. Kan, T. Fukuyama,
Synthesis, 909-917 (2004).

(38) Highly efficient syntesis of medium-sized lactams via intramolecular Staudinger-aza-Wittig reaction of w-azide pentaphenyl ester: synthesis and biological evaluation of LY411575 analogues.
H. Fuwa, Y. Okamura, Y. Morohashi, T. Tomita, T. Iwatsubo, T. Kan, T. Fukuyama and H. Natsuari,
Tetrahedron Lett., 45, 2323-2326 (2004).

(37) Parallel Synthesis of DAPT Derivatives and Their g-Secretase-Inhibitory Activity.
T. Kan, Y. Tominari, K. Rikimaru, Y. Morohashi, H. Natsugari, T. Tomita, T. Iwatsubo and T. Fukuyama,
Bioorg. Med. Chem. Lett.,14, 1983-1985 (2004).

(36) Ns Strategies: A Highly Versatile Synthetic Method for Aminess.
T. Kan,T. Fukuyama,
Chem. Commun., 353-359 (2004).

(35) A Versatile Synthesis of a-Amino Acid Derivatives via the Ugi Four-Component Condensation with a Novel Convertible Isonitrile.
K. Rikimaru, A. Yanagisawa, T. Kan, T. Fukuyama,
Synlett, 41-44 (2004).

(34) Total Synthesis of Potent Antitumor Alkaloid Ecteinascidin 743.
T. Kan,
J. Syn. Org. Chem., Jpn, 61, 949-960 (2003).

(33) Solid-Phase Synthesis of Photoaffinity Probes: Highly Efficient Incorporation of Biotin-tag and Cross-linking group.
T. Kan, Y. Tominari, Y. Morohashi, H. Natsugari, T. Tomita, T. Iwatsubo, T. Fukuyama,
Chem. Commun., 2244-2245 (2003).

(32) Stereocontrolled Total Synthesis of (-)-Ephedradine A (Orantine).
W. Kurosawa, T. Kan, T. Fukuyama,
J. Am. Chem. Soc., 125, 8112-8113 (2003).

(31) Sulindac sulfide is a non-competitive g-secretase inhibitor that preferentially reduces Ab42 generation.
Y. Takahashi, I. Hayashi, Y. Tominari, K. Rikimaru, Y. Morohashi, T. Kan, H. Natsugari, T. Fukuyama, T. Tomita, T. Iwatsubo,
J. Bio. Chem., 278, 18664-18670 (2003).

(30) An Efficient Synthesis of Optically Active trans-2-Aryl-2,3-dihydrobenzofuran-3-carboxylic Acid Esters via C-H Insertion Reaction.
W. Kurosawa, T. Kan, T. Fukuyama,
Synlett, 1028-1030 (2003).

(29) Preparation of Secondary Amines from Primary Amines via 2-Nitrobenzenesulfonamides: N-(4-Methoxybenzyl)-3-phenylpropylamine.
W. Kurosawa, T. Kan, T. Fukuyama,
Org. Synth., 79, 186 (2002).

(28) Highly Versatile Synthesis of Polyamines by the Ns-strategy on a Novel Trityl Chloride Resin.
T. Kan, H. Kobayashi, T. Fukuyama,
Synlett, 1338-1340 (2002).

(27) Efficient Macrocyclization by Means of 2-Nitrobenzenesulfonamide and TotalSynthesis of Lipogrammistin-A.
T. Kan, A. Fujiwara, H. Kobayashi, T. Fukuyama,
Tetrahedron, 58, 6267-6276 (2002).

(26) Total Synthesis of Ecteinascidin 743.
A. Endo, A. Yanagisawa, M. Abe, S. Tohma, T. Kan, T. Fukuyama,
J. Am. Chem. Soc., 124, 6552-6554 (2002).

(25) Efficient Synthesis of Medium-Sized Cyclic Amines by Means of 2-Nitrobenzenesulfonamide.
T. Kan, H. Kobayashi, T. Fukuyama,
Synlett, 697-699 (2002).

(24) Highly Versatile Synthesis of Nitrogen-Containing Compounds by Means of Nitrobenzene-sulfon-amides.
T. Kan, T. Fukuyama,
J. Syn. Org. Chem., Jpn, 59, 779-789 (2001).

(23) Dogger Bank Itch revisited: isolation of (2-hydroxyethyl) dimethylsulfoxonium chloride as a cytotoxic constituent from the marine sponge Theonella aff. Mirabilis.
K. Warabi, Y. Nakao, S. Matsunaga, T. Fukuyama, T. Kan, S. Yokoshima, N. Fusetani,
Comp. Biochem. Physiol., 128B, 27-30, (2001).

(22) Synthesis of Optically Active Arylglycines: Stereoselective Mannich Reaction of Phenols with a New Chiral Template.
S. Tohma, A. Endo, T. Kan, T. Fukuyama,
Synlett, 1179-1181 (2001).

(21) Total Synthesis of Lipogrammistin-A: Efficient Macrocyclization with 2-Nitrobenzene-sulfonamide.
A. Fujiwara, T. Kan, T. Fukuyama,
Synlett, 1667-1669 (2000).

(20) Total Synthesis of Polyamine Toxin HO-416b ang Agel-489 Using a 2-Nitrobenzene-sulfonamide Strategy.
Y. Hidai, T. Kan, T. Fukuyama,
Chem. Pharm. Bull., 48, 1570-1576, (2000).

(19) Hydroxy-Directed, SmI2-Induced Conversion of Carbohydrates into Carbocycles.
T. Kan, S. Nara, T. Ozawa, H. Shirahama, F. Matsuda,
Angew. Chem. Int. Ed., 39, 355 (2000).

(18) N-Carboalkoxy-2-Nitrobenzenesulfonamides: A Practical Preparation of N-Boc-, N-Alloc-, and N-Cbz-Protected Primary Amines.
T. Fukuyama, M. Cheung, T. Kan,
Synlett, 1301-1303 (1999).

(17) Synthetic Study on Ecteinascidin 743 Starting from D-Glucose.
A. Endoh, T. Kan, T. Fukuyama,
Synlett, 1103-1105 (1999).

(16) Total Synthesis of Polyamine Toxin HO-416b Utilizing the 2-Nitrobenzenesulfonamide Protecting Group.
Y. Hidai, T. Kan, T. Fukuyama,
Tetrahedron Lett., 40, 4711 (1999).

(15) Internal Activation of Acrylate-Type Dienophiles in Diels-Alder Reactions. Stereselective Synthesis of Conformationally Constrained Glutamate Analogs.
Y. Ohfune, T. Kan, T. Nakajima,
Tetrahedron, 54. 5207-5224 (1998).

(14) Asymetric Syntheses of 5- and 6-Membered carbocyclic Serine Analogs via an Intermolecular Strecker Synthesis.
Y. Ohfune, K. Nanba, I. Takada, T. Kan, M. Horikawa, T. Nakajima,
Chirality, 9, 459, (1997).

(13) 2,4-Dinitrobenzenesulfonamides: A Simple and Practical Method for the Preparation of Secondary Amines and Diamines.
T. Fukuyama, M. Cheung, C. -K. Jow, Y. Hidai, T. Kan,
Tetrahedron Lett., 38, 5831-5834 (1997).

(12) Efficient Syntheses of Amadori Rearrangement Compounds.
T. Iwamoto, T. Kan, S. Katsumura,Y. Ohfune,
Synlett, 169-170 (1996).

(11) Internal Activation of Acrylate-Type Dienophiles in Diels-Alder Reactions.
T. Kan, Y. Ohfune,
Tetrahedron Lett., 36, 943-946 (1995).

(10) Synthetic Studies on Grayanotoxins. Diastereofacially Selective Dieles-Alder Reaction of 4-Bebzyloxy-2-pentenoate.
T. Kan, M. Oikawa, S. Hosokawa, M. Yanagiya, F. Matsuda, H. Shirahama,
Synlett, 801-804 (1994).

(9) Synthetic Studies on Grayanotoxins. Stereocontrolled Construction of CD-Ring of Grayanotoxins.
T. Kan, M. Oikawa, S. Hosokawa, M. Yanagiya, F. Matsuda, H. Shirahama,
Synlett, 805-808 (1994).

(8) Total Synthesis of (-)-Grayanotoxin(III).
T. Kan, S. Hosokawa, S. Nara, M. Oikawa, S Ito, F. Matsuda, H. Shirahama,
J. Org. Chem., 59, 5532-5534 (1994).

(7) Stereoselective Cyclization Mediated by Samarium(II)Iodide Using Allyl Sulfides and Sulfones as Ketyl Radical Acceptors.
T. Kan, S. Nara, S. Ito, F. Matsuda, H.Shirahama,
J. Org. Chem., 59, 5111-5111 (1994).

(6) Stereocontrolled Construction of B-Ring of Grayanotoxins via Samarium(II) Iodide Promoted Pinacol Coupling Cyclization.
T. Kan, F. Matsuda, M. Yanagiya, H. Shirahama,
Synlett, 391-392 (1991).

(5) Total Synthesis of (+)-Thrsiferol, (+)-Thyrsiferyl 23-Acetate and Venustatriol.
M. Hashimoto, T. Kan, K. Nozaki, M. Yanagiya, H. Shirahama, T. Matsumoto,
J. Org. Chem., 59, 5088-5107 (1990).

(4) Effective Deprotection of 2-(Trimethylsilylethoxy)methlated Alchols (SEM ethers), Synthesis of (+)-Thyrsiferyl 23-Acetate.
T. Kan, M. Hashimoto, M. Yanagiya, H. Shirahama,
Tetrahedron. Lett., 29, 5417-5418 (1988).

(3) Formation of Bicyclo[4.2.0]octane System from Cyclooctenyl Cation Equivalent. Biomimetic Cyclization of Humulene to Protoilludane Derivaties.
T. Takatsu, S. Ito, T. Kan, H. Shirahama, T. Matsumoto,
Synlett, 40-42 (1989).

(2) Total Synthesis of (+)-Thrsiferol and Venustatriol,
M. Hashimoto, T. Kan, K. Nozaki, M. Yanagiya, H. Shirahama, T.Matsumoto,
Tetrahedron Lett., 29, 1143-1144 (1988).

(1) Synthesis of A-B-C-Ring Segment of Thrsiferoll. Construction of a Strained
Tetrahydropyran Ring Existenece as a Boat Form,
M. Hashimoto, T. Kan, M. Yanagiya, H. Shirahama, T. Matsumoto,
Tetrahedron Lett., 28, 5565-5668 (1987).