4.8 Article

Using Chlorotrifluoroethane for Trifluoroethylation of (Hetero)aryl Bromides and Chlorides via Nickel Catalysis

Journal

ORGANIC LETTERS
Volume 23, Issue 4, Pages 1400-1405

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.1c00058

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Funding

  1. National Natural Science Foundation of China [21931013, 21991122]
  2. Strategic Priority Research Program of the Chinese Academy of Sciences [XDB20000000]

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A nickel-catalyzed reductive cross-coupling reaction has been reported for the coupling of industrial chemical CF3CH2Cl with (hetero)aryl bromides and chlorides. The reaction is synthetically simple, exhibits high functional group tolerance, and has been demonstrated to be useful for late-stage modification of pharmaceuticals, providing a convenient route for medicinal chemistry.
A nickel- catalyzed reductive cross-coupling between industrial chemical CF3CH2Cl and (hetero)aryl bromides and chlorides has been reported. The reaction is synthetically simple without the preparation of arylmetals and exhibits high functional group tolerance. The utility of this protocol has been demonstrated by the late-stage modification of pharmaceuticals, providing a facile route for medicinal chemistry.

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