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2015 Fiscal Year Final Research Report

Synthesis of highly substituted chiral arylcyclopropanes via directing group-mediated tertiary C(sp3)-H arylation

Research Project

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Project/Area Number 26860003
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeMulti-year Fund
Research Field Chemical pharmacy
Research InstitutionKyoto Pharmaceutical University

Principal Investigator

Hoshiya Naoyuki  京都薬科大学, 薬学部, 助教 (40566949)

Project Period (FY) 2014-04-01 – 2016-03-31
KeywordsC-H活性化 / シクロプロパン / 芳香環導入
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.

Free Research Field

有機合成

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Published: 2017-05-10  

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