4.5 Article

Nickel-Catalyzed Difluoromethylation of Arylboronic Acids with Bromodifluoromethane

期刊

CHINESE JOURNAL OF CHEMISTRY
卷 36, 期 2, 页码 143-146

出版社

WILEY-V C H VERLAG GMBH
DOI: 10.1002/cjoc.201700624

关键词

arylboronic acids; bromodifluoromethane; cross-coupling; difluoromethylation; nickel

资金

  1. National Natural Science Foundation of China [21425208, 21672238, 21332010, 21421002]
  2. Chinese Academy of Sciences [XDB20000000]
  3. SIOC

向作者/读者索取更多资源

Although bromodifluoromethane (BrCF2H) is a simple and readily available fluorine source, direct formation of difluoromethylated arenes with BrCF2H has not been reported. Herein, we describe an efficient method to access difluoromethylated arenes through a nickel-catalyzed difluoromethylation of arylboronic acids with BrCF2H. The reaction exhibits high efficiency, good functional group tolerance and broad substrate scope, thus providing an efficient route for applications in drug discovery and development. Preliminary mechanistic studies reveal that a difluoromethyl radical is involved in the reaction.

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