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The copper(<scp>ii</scp>)-catalyzed and oxidant-promoted regioselective C-2 difluoromethylation of indoles and pyrroles

Dong Zhang, Zheng Fang, Jinlin Cai, Chengkou Liu, Wei He, Jindian Duan, Na Qin, Zhao Yang, Kai Guo

2020Chemical Communications30 citationsDOI

Abstract

Na) as the source of difluoromethyl groups and a Cu(ii) complex as the catalyst. Various substrates were well tolerated in this transformation and the desired products were obtained in moderate to good yields. Moreover, the late-stage C-2 difluoromethylation of bioactive molecules containing an indole ring was achieved in good yields. Generally, this reaction features excellent functional group compatibility, broad substrate scope and excellent C-2 selectivity.

Topics & Concepts

Indole testChemistryCatalysisRegioselectivityCombinatorial chemistrySelectivityCopperMoleculeFunctional groupOrganic chemistryPolymerFluorine in Organic ChemistryCatalytic C–H Functionalization MethodsCyclopropane Reaction Mechanisms