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Front Cover: Nickel‐Catalyzed 1,1‐Difluoroethylation of (Hetero)aryl Halides with 1,1‐Difluoroethyl Chloride (CH 3 CF 2 Cl) (Asian J. Org. Chem. 3/2020)
Author(s) -
Liu Jianchang,
Zhang Jida,
Li Xiangye,
Wu Chaolin,
Liu Hefu,
Liu Hui,
Sun Fenggang,
Li Yueyun,
Liu Yuying,
Li Xinjin
Publication year - 2020
Publication title -
asian journal of organic chemistry
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.846
H-Index - 44
eISSN - 2193-5815
pISSN - 2193-5807
DOI - 10.1002/ajoc.202000090
Subject(s) - chemistry , aryl , nickel , halide , bioisostere , catalysis , medicinal chemistry , group (periodic table) , functional group , combinatorial chemistry , organic chemistry , chemical synthesis , alkyl , biochemistry , in vitro , polymer
1,1‐Difluoroethylated aromatic compounds are of increasing importance in drug design because the 1,1‐difluoroethyl group (CF 2 CH 3 ) can function as a bioisostere of the methoxy group. Compounds such as those in the accompanying graphic may help combat viruses such as the Coronavirus, which has been affecting Wuhan and the entire world. Herein, we disclose a nickel‐catalyzed 1,1‐difluoroethylation of (hetero)aryl halides with CH 3 CF 2 Cl, an inexpensive and available raw material. The reaction exhibits good functional‐group tolerance and is regarded as a practical method for synthesis of (1,1‐difluoroethyl)arenes. Initial mechanism studies show that a 1,1‐difluoroethyl radical is involved in the current reaction. More information can be found in the Communication by Xinjin Li et al. on page 391 in Issue 3, 2020 (DOI: 10.1002/ajoc.2024).