Difluoromethylation of (hetero)aryl chlorides with chlorodifluoromethane catalyzed by nickel.

ABSTRACT: Relatively low reactivity hinders using chlorodifluoromethane (ClCF2H) for general difluoromethylation with organic molecules, despite its availability as an inexpensive industrial chemical. To date, transformations of ClCF2H are very limited and most of them involve difluorocarbene intermediate. Here, we describe a strategy for difluoromethylation of aromatics through nickel-catalyzed cross-coupling of ClCF2H with readily accessible (hetero)aryl chlorides. The reaction proceeds under mild reaction conditions with high efficiency and features synthetic simplicity without preformation of arylmetals and broad substrate scope, including a variety of heteroaromatics and commercially available pharmaceuticals. The reliable practicability and scalability of the current nickel-catalyzed process h

SUBMITTER: Xu C 

PROVIDER: S-EPMC5862906 | biostudies-literature | 2018 Mar

REPOSITORIES: biostudies-literature