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Palladium-catalyzed difluoromethylation of heteroaryl chlorides, bromides and iodides†
Changhui Lu,Yang Gu,Jiang Wu,Yucheng Gu,Qilong Shen
Chemical Science Pub Date : 04/24/2017 00:00:00 , DOI:10.1039/C7SC00691H
Abstract

A palladium-catalyzed difluoromethylation of a series of heteroaryl chlorides, bromides and iodides under mild conditions is described. A wide range of heteroaryl halides such as pyridyl, pyrimidyl, pyrazyl, funanyl, thienyl, pyazolyl, imidazolyl, thiazolyl, and oxazolyl halides were efficiently difluoromethylated, thus providing medicinal chemists an alternative choice for the preparation of drug candidates with the difluoromethylated heteroarene unit.

Graphical abstract: Palladium-catalyzed difluoromethylation of heteroaryl chlorides, bromides and iodides
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