| Project/Area Number |
26460168
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Microbial Chemistry Research Foundation |
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Principal Investigator |
WATANABE Takumi 公益財団法人微生物化学研究会, 微生物化学研究所, 部長 (80270544)
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| Co-Investigator(Renkei-kenkyūsha) |
ISHIZAKI Yoshimasa (公財)微生物化学研究会, 微生物化学研究所 第2生物活性研究部, 主任研究員 (10414103)
UMEZAWA Yoji (公財)微生物化学研究会, 微生物化学研究所 分子構造解析部, 部長 (60160313)
SAKAMOTO Shuichi (公財)微生物化学研究会, 微生物化学研究所 沼津支所, 上級研究員 (60346070)
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| Research Collaborator |
Gandamala Ravi (公財)微生物化学研究会, 微生物化学研究所 有機合成研究部, 博士研究員
Wang Lu (公財)微生物化学研究会, 微生物化学研究所 有機合成研究部, 博士研究員
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| Project Period (FY) |
2014-04-01 – 2017-03-31
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| Project Status |
Completed (Fiscal Year 2016)
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| Budget Amount *help |
¥5,070,000 (Direct Cost: ¥3,900,000、Indirect Cost: ¥1,170,000)
Fiscal Year 2016: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2014: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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| Keywords | 触媒的不斉合成 / ケミカルバイオロジー / XDR-TB / 抗結核薬 / 構造活性相関 |
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| Outline of Final Research Achievements |
Initially, caprazamycin derivatives which is not accessible by semi-synthetic strategy starting from naturally-occurring captazamycin were prepared based on the catalytic asymmetric synthetic route to caprazol and caprazamycin; caprazol derivatives with longer aliphatic side chain installed on one of the nitrogen atoms embedded in the seven-membered lactam core were successfully synthesized.
Then, catalytic asymmetric synthesis of CPZEN-45 was accomplised. In the synthetic route, a complex comprising Zn and chiral linked-BINOL ligand was found to be effective for the aldol reaction to construct the beta-hydroxyamino acid substructure to show excellent diastereoselectivity.
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