2021 Fiscal Year Final Research Report
Development of synthetic pathways and syntheses of natural products applicable to novel biological activity evaluation research
| Project/Area Number |
19K06981
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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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| Review Section |
Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
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| Research Institution | Hoshi University |
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Principal Investigator |
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| Project Period (FY) |
2019-04-01 – 2022-03-31
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| Keywords | 天然有機化合物 / 全合成 / caseabalansin A / hapromintrin B / mollolide A / cochlearol B / parvistemonine A / lamellodysidine A |
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| Outline of Final Research Achievements |
The total synthesis of caseabalansin A, that possesses a tetracyclic nucleus was achieved. Since the total synthesis of caseabalansin A was completed early, we conducted synthetic studies on cochlearol B with a pentacyclic skeleton, parvistemonine A with a tricyclic skeleton, corallocin A with a benzofuran skeleton, and lamellodysidine A with a tetracyclic skeleton. As a result of the implementation, synthetic pathways of these four natural products were established as well.
For hapromintrin B, which has a hexacyclic skeleton, we have succeeded in the construction of the tetracyclic skeleton so far. Currently, we are continuing to develop a synthetic pathway for hapromintrin B, including a geminal dimethyl units. For mollolide A, which has a bicyclo [3.2.1] octane ring, we succeeded in synthesizing the core skeleton. In addition, we are conducting the synthesis in optically active form and the improvement of synthetic yields, to furnish total synthesis.
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| Free Research Field |
有機合成化学
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| Academic Significance and Societal Importance of the Research Achievements |
本研究において全合成経路を確立したcaseabalansin A、cochlearol B、parvistemonine A、corallocin Aおよびlamellodysidine A、そして合成検討中のhapromintrin Bおよびmollolide Aは、それぞれ全く異なる骨格を有している。いずれの全合成経路も、短工程、高収率であり、創薬化学研究への適用が可能と考えられる。本研究において開発した合成経路を利用して誘導体合成を実施し、標的タンパク質の、新規モジュレーターが見出されることを期待している。また、開発した合成手法が、有機合成化学の進展に寄与するものと考えられる。
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