Synthesis of highly substituted chiral arylcyclopropanes via directing group-mediated tertiary C(sp3)-H arylation
| Project/Area Number |
26860003
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Chemical pharmacy
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| Research Institution | Kyoto Pharmaceutical University |
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Principal Investigator |
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| Project Period (FY) |
2014-04-01 – 2016-03-31
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| Project Status |
Completed (Fiscal Year 2015)
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| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2015: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2014: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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| Keywords | C-H活性化 / シクロプロパン / 芳香環導入 / C-H官能基化 / 不斉４級炭素 / 三次元的多様性 / 配座制御 |
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| Outline of Final Research Achievements |
In this research, functionalization of tertiary C(sp3)-H via catalytic C-H activation was investigated and Pd-catalyzed arylation and alkylation of tertiary C(sp3)-H bond were successfully developed. This is the first report of functionalization of tertiary C(sp3)-H via Pd-catalyzed C-H activation. The novel Pd-catalyzed functionalization provided alternative routes to chiral arylcyclopropanes and alkylcyclopropanes which are attractive candidates for new medicinal compounds. Now transition metal-catalyzed amination and alkoxylation of tertiary C-H bond on chiral cyclopropanes are under investigation.
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Report
(3 results)
Research Products
(9 results)
