Curriculum Vitae Hidetsura CHO (長 秀連), Professor, Dr. Graduate School of Science and Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Japan Date and Place of Birth: June 4, 1949, Fukuoka, Japan Nationality: Japanese Address (Office): 6-3, Aoba, Aramaki, Aoba-ku, Sendai, 980-8578, Japan.
E-mail: hcho@mail.pharm.tohoku.ac.jp Tel. +81-(0)80-1424-2230 (private)
Tel. +81-22-795-5501 (office), Fax. +81-22-795-5502 (office)
Address (Home): (1) 1-18-5, Kitakasugaoka, Ibaraki-shi, Osaka, 567-0048, Japan. (2) 405, Kaluo Johzenji-dohri, 1-15-10, Honcho, Aobaku, Sendai,
E-mail: kochoran@qj8.so-net.ne.jp, Tel. +81-(0)90-4760-5633 (home)
Education: Apr. 1969-Mar. 1973 Kyoto University (Department of Pharmaceutical Sciences) Apr. 1978-Mar. 1978 Kyoto University (Prof. Y. Inubushi, Graduate School of
Oct. 1978-Sept. 1979 Iowa State University (Post-doctor, Prof. G. A. Kraus,
Oct. 1979-Sept. 1980 Harvard Univerity (Post-doctor, Prof. E. J. Corey,
Professional Works: Dec. 1980-Dec. 1992 Suntory Institute (Senior Researcher, Research Institute for
Jan. 1993-Jun. 1996 Japan Tobacco Inc. (Group Leader, Medicinal Chemistry
Laboratories, Central Pharmaceutical Research Institute)
July 1996-May 2000 Japan Tobacco Inc. (Dupty Director, Medicinal Chemistry
Laboratories, Central Pharmaceutical Research Institute)
Jun. 2000-July 2002 Japan Tobacco Inc. (Director, Product Development
Laboratories, Central Pharmaceutical Research Institute)
Aug. 2002-Mar. 2008 Japan Tobacco Inc. (Vice-President, Central Pharmaceutical
Apr. 2008-now Tohoku University (Professor, Graduate School of Science and
Graduate School of Pharmaceutical Sciences)
(July 2003-Dec. 2012 Member of Board of Directors in Japanese Society for Process
Research Subjects: 1. Development of novel synthetic methods for heterocyclic compounds and molecular
2. Studies on synthesis of RNA-binding small molecules for HCV-IRES (hepatitis C
3. Studies on synthesis of class III-compounds passing through the peptide transporter. Award: The Award for Promotional and Excellent Research of Synthetic Organic Chemistry (The Society of Synthetic Organic Chemistry, Japan, in 1988). “Synthetic Studies on Novel Dihydropyrimidine Derivatives” Representative 29 Publications (Total 41) plus 2 Textbooks: [1] H. Cho, Y. Iwama, K. Okano, H. Tokuyama Construction of Dibenzazocine Skeleton by Regiocontrolled Ring-Expansion Reaction of Cyclic Oxime with DIBAL-H: Facile Synthesis of 17β-Hydroxysteroid Dehydrogenase Type 3 Inhibitor
SYNLETT, 2013, 24, 813-816. [2] H. Cho, Y. Iwama, N. Mitsuhashi, K. Sugimoto, K. Okano, H. Tokuyama Ring-Expansion Reaction of Oximes with Aluminum Reductants Molecules, 2012, 17, 7348-7355. [3] Y. Nishimura, Y. Yasui, S. Kobayashi, M. Yamaguchi, H. Cho Synthesis of novel 2-phenyl-5-substituted dihydropyrimidines using 2-phenyl-1,3-diaza-1,3-butadienes and electron-deficient olefins Tetrahedron, 2012, 68, 3342-3350. [4] H. Cho, Y. Nishimura, Y. Yasui, M. Yamaguchi Construction of Dihydropyrimidine Skeleton Using 1,2,4-Trisubstituted-1,3-Diaza- Tetrahedron Letters, 2012, 53, 1177-1179 [5] H. Cho, E. Kwon, Y. Yasui, S. Kobayashi, S. Yoshida, Y. Nishimura, M.Yamaguchi Ring Cleavage of Dihydropyrimidine skeleton Tetrahedron Letters, 2011, 52, 7185-7188. [6] H. Cho, Y. Yasui, S. Kobayashi, E. Kwon, M. Arisawa, M.Yamaguchi, Synthesis and Substitution Reactions of 4(6)-Chlorodihydropyrimidines Heterocycles, 2011, 83 (8), 1807-1818. [7] H. Cho, Y. Nishimura, Y. Yasui, S. Kobayashi, S. Yoshida, E. Kwon, M. Yamaguchi, Synthesis of 4-Unsubstituted Dihydropyrimidines. Nucleophilic Substitution at Position-2 of Dihydropyrimidines., Tetrahedron, 2011, 67, 2661-2669. [8] H. Cho, K. Sugimoto, Y. Iwama, N. Mitsuhashi, K.Okano, H.Tokuyama, Regiospecific Rearrangement of Hydroxylamines to Secondary Amines Using Diisobutylaluminum Hydride, Heterocycles, 2011, 82, 1633-1644. [9] H. Cho, Y. Iwama, K. Sugimoto, S. Mori, H. Tokuyama, Regioselective Synthesis of Heterocycles Containing Nitrogen Neighboring an Aromatic Ring by Reductive Ring Expansion Using Diisobutylaluminum Hydride (DIBALH) and Studies on the Reaction Mechanism, J. Org. Chem.,2010,75, 627-636. [10] H. Cho, Y. Iwama, K. Sugimoto, E. Kwon, H.Tokuyama, Regiospecific synthesis of unsubstituted basic skeletons of heterocycles containing nitrogen neighboring an aromatic ring by the reductive ring expansion reaction using diisobutylaluminum hydride, Heterocycles, 2009, 78, 1183-1190. [11] H. Ueno, K. Yokota, J. Hoshi, K. Yasue, M. Hayashi, Y. Hase, I. Uchida, K. Aisaka, S. Katoh, H. Cho, Synthesis of structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring, J. Med. Chem., 2005, 48, 3586-3604. [12] H. Ueno, K. Yokota, J. Hoshi, K. Yasue, M. Hayashi, I. Uchida, K. Aisaka, Y. Hase, S. Katoh, H. Cho, Discovery of novel tetrahydroisoquinoline derivatives as potent and selective factor Xa inhibitors, Bioorg. & Med. Chem. Lett., 2005, 15, 185-189. [13] H. Ueno, S. Katoh, K. Yokota, J. Hoshi, M. Hayashi, I. Uchida, K. Aisaka, Y. Hase, H. Cho, Structure-activity relationships of potent and selective factor Xa inhibitors: benzimidazole derivatives with the side chain oriented to the prime site of factor Xa, Bioorg. & Med. Chem. Lett., 2004, 14, 4281-4286. [14] H. Cho, K. Murakami, H. Nakanishi, A. Fujisawa, H. Isoshima, M. Niwa, K. Hayakawa, Y. Hase, I. Uchida, H. Watanabe, K. Wakitani, K. Aisaka, Synthesis and Structure-Activity Relationships of 5,6,7,8-Tetrahydro-4H-thieno[3,2-b]azepine Derivatives: Novel Arginine Vasopressin Antagonists, J. Med. Chem., 2004, 47,
101-109. [15] H. W. Hamilton, G. Nishiguchi, S. E. Hagen, J. D. Domagala, P. C. Weber, S. Gracheck, S. L. Boulware, E. C. Nordby, H. Cho, T. Nakamura, W. Watanabe, S. Ikeda, Novel benzthiodiazepines as antiherpetic agents: SAR improvement of therapeutic index by alternations of the 7-membered ring, Bioorg. & Med. Chem. Lett.,
2002, 12, 2981-2983. [16] T. Inaba, Y. Yamada, H. Abe, S. Sagawa, H. Cho, (1S)-1-[(4R)-2,2-dimethyl-1,3- dioxolan-4-yl]-2-hydroxyethylammonium benzoate, a versatile building block for chiral 2-aminoalkanols: concise synthesis and application to Nelfinavir, a potent HIV protease inhibitor, J. Org. Chem., 2000, 65, 1623-1628. [17] H. Cho, K. Murakami, A. Fujisawa, M. Niwa, H. Nakanishi, I. Uchida, Synthesis of novel 5,6,7,8-tetrahydro-4H-thieno[2,3-b][1,4]diazepine derivatives, Heterocycles, 1998, 48, 1555-1566. [18] H. Cho, K. Murakami, H. Nakanishi, H. Isoshima, K. Hayakawa, I. Uchida, Regioselective synthesis of several heterocyclic fused azepines using
diisobutylaluminum hydride, Heterocycles, 1998, 48, 919-927. [19] H. Cho, S. Matsuki, A. Mizuno, H. Annoura, T. Tatsuoka, Synthesis of pyrroloazepines. Facile synthesis of 2-substituted pyrrole derivatives by the phosgene method, J. Heterocyclic Chem., 1997, 34, 87-91. [20] H. Cho, S. Kato, S. Sayama, K. Murakami, H. Nakanishi, Y. Kajimoto, H. Ueno, H. Kawasaki, K. Aisaka, I. Uchida, Synthesis and selective coronary vasodilative activity of JTV-506 and 3,4-dihydro-2,2-bis(methoxymethyl)-2H-1-benzopyran-3-ol derivatives, potassium channel openers, J. Med. Chem., 1996, 39, 3797-3805. [21] H. Cho, S. Matsuki, Ring construction of several heterocycles with phosphorus pentoxide-methanesulfonic acid (PPMA), Heterocycles, 1996, 43, 127-131. [22] H. Cho, M. Ueda, M. Tamaoka, M. Hamaguchi, K. Aisaka, Y. Kiso, T. Inoue, R. Ogino, T. Tatsuoka, T. Ishihara, T. Noguchi、 I. Morita, S. Murota, Novel caffeic acid derivatives: Extremely potent inhibitors of 12-lipoxygenase, J. Med. Chem., 1991, 34, 1503-1505. [23] H.Cho, M. Ueda, K. Shima, A. Mizuno, M. Hayashimatsu, Y. Ohnaka, Y. Takeuchi, M. Hamaguchi, K. Aisaka, T. Hidaka, M. Kawai, M. Takeda, T. Ishihara,K. Funahashi, F. Satoh, M. Morita, T. Noguchi, Dihydropyrimidines: Novel calcium antagonists with potent and long-lasting vasodilative and antihypertensive activity, J. Med. Chem., 1989, 32, 2399-2406. [24] H. Cho, T. Iwashita, M. Ueda, A. Mizuno, K. Mizukawa, M. Hamaguchi, On the tautomerism of dihydropyrimidines: The influence of the 2- and 5-substituents on the
observation of tautomers, J. Am. Chem. Soc., 1988, 110, 4832-4834. [25] H. Cho, K. Shima, M. Hayashimatsu, Y. Ohnaka, A. Mizuno, Y. Takeuchi, Synthesis of novel dihydropyrimidines and tetrahydropyrimidines, J. Org. Chem., 1985, 50, 4227-4230. [26] G. A. Kraus, H. Cho, S. Crowley, B. Roth, H. Sugimoto, S. Prugh, Phthalide annulation: The synthesis of kalafungin, pachybasin, and chrysophanol, J. Org. Chem., 1983, 48, 3439-3444. [27] E. J. Corey, H. Cho, C. Rucker, D. H. Hua, Studies with trialkylsilyltriflates: new syntheses and applications, Tetrahedron Lett., 1981, 22, 3455-3458. [28] E. J. Corey, L. O. Weigel, A. R. Chamberlin, H. Cho, D. H. Hua, Total synthesis of Maytansine, J. Am. Chem. Soc., 1980, 102, 6613-6615. [29] T. Harayama, H. Cho, Y. Inubushi, Total synthesis of dl-chamaecynone, a termiticidal norsesquiterpene, Tetrahedron Lett., 1977, 3273-3276. [Textbook] [1] Pharmaceutical Process Chemistry (Kagakudoujin INC/The Japanese Society for Process Chemistry, <in Japanese>, published in April 1, 2005, for beginners of Process Chemistry Division) [2] Pharmaceutical Sciences; Discovery and Development of New Medicines (Nanzandou INC, August 25, 2012) Hobby: Classic music, Opera, Operetta, Musical, Kabuki, Golf, Go.
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