| Project/Area Number |
08672459
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Chemical pharmacy
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| Research Institution | Kyoto Pharmaceutical University |
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Principal Investigator |
AKAJI Kenichi Kyoto Pharmaceutical Univ.Department of Pharmaceutical Scineces, Associate Professor, 薬学部, 助教授 (60142296)
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| Co-Investigator(Kenkyū-buntansha) |
KIMURA Tooru Kyoto Pharmaceutical Univ.Department of Pharmaceutical Scineces, Instructor, 薬学部, 助手 (70204980)
FUJIWARA Yoichi Kyoto Pharmaceutical Univ.Department of Pharmaceutical Scineces, Instructor, 薬学部, 助手 (60199396)
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| Project Period (FY) |
1996 – 1997
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| Project Status |
Completed (Fiscal Year 1997)
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| Budget Amount *help |
¥2,500,000 (Direct Cost: ¥2,500,000)
Fiscal Year 1997: ¥900,000 (Direct Cost: ¥900,000)
Fiscal Year 1996: ¥1,600,000 (Direct Cost: ¥1,600,000)
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| Keywords | coupling reagent / anti-cancer alkaloid / mirabazole / dialkyl amino acid / thiazoline |
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| Research Abstract |
Convergent synthesis of (-) Mirabazole C and B,tetra thiazoline/thiazole alkaloids isolated from Blue-Green Alga, have been achieved. The successive thiazoline rings of (-) mirabazole C and B were formed by a single step cyclization mediated by TiC14 treatment of a tripeptideamide intermediates. Convergent synthesis of the key intermediates derived from three 2-methylcysteine residues was first achieved using a newly developed coupling reagent, 2-chloro-1,3-dimethylimidazolidium hexafluorophosphate (CIP). The effectiveness of CIP for the coupling of alpha, alpha-dialkyl amino acids and the reaction pathway of the activation were clarified by the syntheses of model pepitdes containing alpha, alpha-dimethylamino acid.
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