Synthetic studies of alkaloids possessing iNOS inducing activities
| Project/Area Number |
18K06558
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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 | Toho University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
加藤 恵介 東邦大学, 薬学部, 教授 (80276609)
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| Project Period (FY) |
2018-04-01 – 2021-03-31
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| Project Status |
Completed (Fiscal Year 2020)
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| Budget Amount *help |
¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2020: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2019: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2018: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
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| Keywords | 全合成 / 天然物 / アルカロイド / iNOS / ウルポシジン / NO / 一酸化窒素 |
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| Outline of Final Research Achievements |
Synthesis of urupocidin A was examined. The left segment of urupocidine A was synthesized stereoselectively starting from 4-octynoic acid via coupling with the acetylide, asymmetric reduction, trans reduction, epoxidation, reduction of the epoxide and oxidation. The lactone intermediate possessing the framework and asymmetric centers of the left segment was obtained. On the other hand, the right segment was synthesized via Keck asymmetric allylation, mesylation and Gabriel syntheses.
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| Academic Significance and Societal Importance of the Research Achievements |
最近単離構造決定され医薬品リード化合物として期待されるウルポシジンAをとり上げ、これらの独自の方法論に基づく初の全合成達成を本研究の目的と定め研究を展開した。その結果、今後の展開に重要と思われる左右両フラグメントを合成することができ、本研究によりウルポシジン及びその誘導体の化学合成を可能とする端緒を見いだすことができた。
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Report
(4 results)
Research Products
(15 results)
