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Palladium-catalyzed difluoromethylation of heteroaryl chlorides, bromides and iodides

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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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Publication details

The article was received on 14 Feb 2017, accepted on 19 Apr 2017 and first published on 24 Apr 2017


Article type: Edge Article
DOI: 10.1039/C7SC00691H
Citation: Chem. Sci., 2017, Advance Article
  • Open access: Creative Commons BY license
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    Palladium-catalyzed difluoromethylation of heteroaryl chlorides, bromides and iodides

    C. Lu, Y. Gu, J. Wu, Y. Gu and Q. Shen, Chem. Sci., 2017, Advance Article , DOI: 10.1039/C7SC00691H

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