2013 Fiscal Year Final Research Report
Synthetic studies of bioactive molecules based on microwave assisted ring formation and fragmentation reaction
| Project/Area Number |
23590021
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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 |
Chemical pharmacy
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| Research Institution | Meiji Pharmaceutical University |
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Principal Investigator |
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| Project Period (FY) |
2011 – 2013
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| Keywords | マイクロ波 / 環開裂 / ビシクロ環 / ザラゴジン酸 / ホマクチン |
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| Research Abstract |
The synthetic studies of zaragozic acid A, phomactin and paclitaxel by using of microwave heating and the fragmentation reaction of bridged bicyclic compound were performed. The following results were obtained. 1. The complete synthesis of the core part of zaragozic acid was achieved by the efficient fragmentation and re-cyclization from the bicyclic compound with acetal bridging. 2. The new zaragozic acid analog, squalene synthase inhibitor, was synthesized. 3. The construction method for the six-membered ring moiety, involving the four consecutive asymmetric carbon, in phomactin was developed by the retro-aldol fragmentation reaction of the bridged bicyclic compound and the later epimerization.
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