Total Synthesis of Nitrogen-containing Macrocyclic Natural Products Useful for Drug Discovery
| Project/Area Number |
16H05074
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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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 | Nagasaki University |
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Principal Investigator |
HATAKEYAMA Susumi 長崎大学, 先端創薬イノベーションセンター, 教授 (20143000)
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| Co-Investigator(Kenkyū-buntansha) |
石原 淳 長崎大学, 医歯薬学総合研究科(薬学系), 教授 (80250413)
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| Project Period (FY) |
2016-04-01 – 2019-03-31
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| Project Status |
Completed (Fiscal Year 2018)
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| Budget Amount *help |
¥17,940,000 (Direct Cost: ¥13,800,000、Indirect Cost: ¥4,140,000)
Fiscal Year 2018: ¥5,720,000 (Direct Cost: ¥4,400,000、Indirect Cost: ¥1,320,000)
Fiscal Year 2017: ¥5,850,000 (Direct Cost: ¥4,500,000、Indirect Cost: ¥1,350,000)
Fiscal Year 2016: ¥6,370,000 (Direct Cost: ¥4,900,000、Indirect Cost: ¥1,470,000)
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| Keywords | 有機合成化学 / 天然物 / 全合成 / 天然部 |
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| Outline of Final Research Achievements |
We have studied on the total synthesis of natural products having intriguing nitrogen-containing macrocyclic structures and biological activities useful for drug discovery. As a result, we have achieved the formal synthesis of haliclonin A. In addition, we have developed a useful method for the preparation of the key precursor for the synthesis of marineosins A and B. We have also developed highly stereocontrolled routes to C4-C9 and C10-C21 fragments of thermolide family of natural products.
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| Academic Significance and Societal Importance of the Research Achievements |
本研究は、特異な含窒素大員環構造と抗腫瘍活性や抗菌活性や抗線虫活性などの顕著な生物活性を持つ天然物を合成標的としており、医薬開発に繋がる多様な分子の供給という観点から、社会的意義を持つ。また、本基盤研究期間中に開発した連続的なタンデムラジカル反応を基軸とするビシクロ環合成法やキナアルカロイドを有機触媒として用いる不斉反応に基づくポリプロピオネートの一般合成法は、これまでに前例がなく、学術的意義を持つ。
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Report
(4 results)
Research Products
(43 results)
