| Project/Area Number |
17K08205
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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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| Research Field |
Chemical pharmacy
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| Research Institution | Chiba University |
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Principal Investigator |
Arai Shigeru 千葉大学, 大学院薬学研究院, 准教授 (20285224)
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| Project Period (FY) |
2017-04-01 – 2020-03-31
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| Project Status |
Completed (Fiscal Year 2019)
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| Budget Amount *help |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2019: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2018: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2017: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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| Keywords | 遷移金属触媒 / アレン / ニッケル / コバルト / 選択的化学合成 / 環化付加反応 / アルカロイド / 環化反応 / シアノ化 / 合成化学 / 触媒反応 / 有機化学 / ヘテロ環 |
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| Outline of Final Research Achievements |
Heterocycles are significant units for drug and their candidates, therefore their simple and efficient synthesis have been key issue in synthetic organic chemistry. One of the most powerful solutions is a new strategy that enables both regio- and stereoselective functionalization and quick construction of carbon skeleton through a single operation. The author focused on allene with transitions metal catalysis that provides a new methodology for highly functionalized hetero- and carboxylic compounds. In the case of nickel catalysis, various methods such as [2+2+2], [4+2], [2+2] cycloadditions have been successfully developed. Origin of the higher selectivity observed in their reactions is the critical discrimination of allenyl C=C bonds during the transformation. On the other hand, coal catalysis revealed that examines are suitable substrates to give carboradical species, and the electron deficient aromatic ring selectively react to form lactams under mild conditions.
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| Academic Significance and Societal Importance of the Research Achievements |
本研究では、医薬品に頻繁に見られる複素環化合物を簡単かつ迅速に組み上げる新技術を確立した。安価なニッケル触媒を用いて２環性構造を１工程で創ることに成功し、コバルト触媒系では、芳香族化合物を直接利用して環状分子を構築する新手法の開発に成功した。いずれの手法も、実用性が高く環境調和性にも優れている。本手法を用いて、医薬農薬や生命科学研究に用いられる生物活性分子の簡便供給に有用と考えられる。
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