Development of synthetic strategies towards bioactive polycyclic natural products via catalytic radical cascade transformations
Project/Area Number |
18K06578
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Research Category |
Grant-in-Aid for Scientific Research (C)
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Allocation Type | Multi-year Fund |
Section | 一般 |
Review Section |
Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
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Research Institution | Okayama University |
Principal Investigator |
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Project Period (FY) |
2018-04-01 – 2022-03-31
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Project Status |
Completed (Fiscal Year 2021)
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Budget Amount *help |
¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2020: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2019: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2018: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
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Keywords | ラジカル反応 / 天然物 / カスケード反応 / 多環性分子骨格 / レドックス / 抗ウイルス活性 / 全合成 / カスケード / キノンレドックス / 可視光レドックス触媒 / 創薬 / 生物活性天然物 / 有機合成化学 / 可視光励起触媒 |
Outline of Final Research Achievements |
In the present study, we developed new radical cascade reactions that feature environmentally-benign catalytic chemical transformations with high energy efficiency to produce polycyclic organic molecules. In addition, we devised synthetic routes to bioactive natural products based on the radical cascade reactions; 1) the formal total synthesis of antiviral marine natural product hamigeran B was accomplished by a visible-light-mediated radical cascade transformation; 2) a new means for accessing a hydroxybenzofuran from an alkynylquinone under quinone-hydroquinone organic redox conditions was developed, enabling the total synthesis of liphagal, a natural PI3kα inhibitor.
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Academic Significance and Societal Importance of the Research Achievements |
我々は、医薬資源天然物の人工合成に欠かせない化学反応プロセスの低環境負荷・省エネルギー化に向けた研究を行った。その結果、可視光照射によって連続的に進行する化学反応や生体内酸化還元過程を模倣した化学反応を開発し、これらの反応を組み込んだ医薬資源天然物の新しい合成方法を確立することができた。本成果は、創薬・化学産業をはじめ、有機物質の創製に関わる広い分野の発展に寄与することが期待される。
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Report
(3 results)
Research Products
(18 results)
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[Journal Article] Ru(II)-Catalyzed C-H Aminocarbonylation of N-(Hetero)aryl-7-azaindoles with Isocyanates2018
Author(s)
Jeong, T.; Lee, S.-H.; Chun, R.; Han, S.; Han, S.-H.; Jeon, Y.-U.; Park, J.; Yoshimitsu, T.; Mishra, N. K.; Kim, I.-S.
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Journal Title
J. Org. Chem.
Volume: 83
Issue: 8
Pages: 4641-4649
DOI
Related Report
Peer Reviewed / Int'l Joint Research
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[Journal Article] Visceral Adipose Tissue Drives Cardiac Aging Through Modulation of Fibroblast Senescence by Osteopontin Production2018
Author(s)
Sawaki D.; Czibik G.; Pini, M.; Ternacle, J.; Suffee, N.; Mercedes, R.; Marcelin, G.; Surenaud, M.; Marcos, E.; Gual. P.; Clement, K.; Hue, S.; Adnot, S.; Hatem, N. S.; Tsuchimochi, Y.; Yoshimitsu, T.; Henegar, C.; Derumeaux, G.
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Journal Title
Circulation
Volume: -
Issue: 8
Pages: 809-822
DOI
Related Report
Peer Reviewed / Int'l Joint Research
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