| Project/Area Number |
18K14871
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| Research Category |
Grant-in-Aid for Early-Career Scientists
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| Allocation Type | Multi-year Fund |
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| Review Section |
Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
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| Research Institution | Gifu Pharmaceutical University |
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Principal Investigator |
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| Project Period (FY) |
2018-04-01 – 2020-03-31
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| Project Status |
Completed (Fiscal Year 2019)
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| Budget Amount *help |
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2019: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2018: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
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| Keywords | 有機金属化学 / Ni / カルボニル付加反応 / Grignard反応 / 還元的カップリング / 有機金属錯体 / ニッケル |
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| Outline of Final Research Achievements |
In this study, a reductive carbonyl arylation reaction using a nickel catalyst was investigated. The reaction proceeded efficiently by using a NiCl2 bpy) complex. The highly active nickel center at this time is considered to be electronically stabilized by the diimine-based ligand and NaI. This highly active species allowed the reaction to proceed with more than 30 substrates. Most of them had a yield of over 80%, and were applicable to substrates that were difficult to use in the past, such as substrates containing esters and ketones and hydroxyl groups serving as proton sources. Moreover, the application to enantioselective reaction has been found by using an asymmetric ligand.
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| Academic Significance and Societal Importance of the Research Achievements |
本研究ではGrignard反応の持つ、100年の歴史を打ち破る触媒的Grignard型反応の実現を目指し研究を遂行する。よってこれらの欠点を克服し、系中で触媒量の求核性化学種の生成を伴う触媒的Grignard型反応の開発は、医薬品の合成戦略を拡大するものである。本研究目的は新奇反応性を有する触媒反応の開発を通し、持続可能な化学の実現と医薬品製造(ものづくり)における問題点の克服を同時に達成するものである。
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