4.5 Article

Nickel-Catalyzed Reductive Cross-Coupling of (Hetero)aryl Halides with 2-Chloro-1,1-difluoroethane: Facile Access to 2,2-Difluoroethylated Aromatics

Journal

ASIAN JOURNAL OF ORGANIC CHEMISTRY
Volume 11, Issue 6, Pages -

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/ajoc.202200169

Keywords

aryl halides; 2; 2-difluoroethylation; fluorine; nickel; reductive coupling

Funding

  1. National Natural Science Foundation of China [22101157]
  2. Natural Science Foundation of Shandong Province [ZR2019LFG008]
  3. open project foundation of Key Laboratory of Organofluorine Chemistry, Chinese Academy of Sciences

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A mild and efficient method for the synthesis of 2,2-difluoroethylated (hetero)aryl halides using readily available 2-chloro-1,1-difluoroethane has been developed. The reductive cross-coupling reaction is synthetically simple and exhibits good functional group tolerance. This approach provides a facile access to synthesize 2,2-difluoroethylated molecules for drug discovery.
A mild and efficient nickel-catalyzed 2,2-difluoroethylation of (hetero)aryl halides with readily available 2-chloro-1,1-difluoroethane has been developed. The reductive cross-coupling reaction is synthetically simple and exhibits good functional group tolerance. This approach provides a facile access to synthesize 2,2-difluoroethylated molecules for drug discovery.

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