Development of the aryne generation method via dual activation and of cascade reaction using unstable chemical species
| Project/Area Number |
15K07879
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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 | Hyogo University of Health Sciences |
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Principal Investigator |
YOSHIOKA Eito 兵庫医療大学, 薬学部, 講師 (80435685)
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| Project Period (FY) |
2015-04-01 – 2019-03-31
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| Project Status |
Completed (Fiscal Year 2018)
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| Budget Amount *help |
¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2018: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2017: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2016: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2015: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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| Keywords | ベンザイン / ラジカル / 二重活性化 / 鉄触媒 / 可視光励起触媒 / 鉄試薬 / 光励起触媒 / ベンザイン前駆体 / [2+2]型反応 / C-N結合挿入反応 / 酸化反応 / 光触媒 / 一電子移動 |
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| Outline of Final Research Achievements |
I studied the following reactions using unstable chemical species such as aryne or radical for developing rapid and/or efficient reactions. The aryne generation from its precursor was improved. I also reported new one-pot synthesis of xanthene and benzodiazepine via the insertion reaction of aryne into the C=O p-bond or C-N s-bond. The reactions using organic photo-catalyst or iron reagents were developed.
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| Academic Significance and Societal Importance of the Research Achievements |
不安定化学種は、反応制御に困難が伴う一方、新規反応の開発や標的分子合成の効率化が期待できる。ベンザインは、所望の二置換ベンゼンや複素環を合成できる有用な化学種であり、その発生の改良は当該分野の根幹として広くボトムアップに繋がる。また、多環性複素環類の合成や複素環の特性を生かした新規反応開発は、生物活性物質を始めとする医薬品シーズやライブラリ構築に繋がる。ラジカル研究について、部位選択的な反応やカスケード反応の開発も医薬品シーズやライブラリ構築に不可欠なプロセスの提供に繋がる。
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Report
(5 results)
Research Products
(32 results)
