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1,1-Difluoroethyl chloride (CH3CF2Cl), a novel difluoroalkylating reagent for 1,1-difluoroethylation of arylboronic acids.


ABSTRACT: 1,1-Difluoroethylated aromatics are of great importance in medicinal chemistry and related fields. 1,1-Difluoroethyl chloride (CH3CF2Cl), a cheap and abundant industrial raw material, is viewed as an ideal 1,1-difluoroethylating reagent, but the direct introduction of the difluoroethyl (CF2CH3) group onto aromatic rings using CH3CF2Cl has not been successfully accomplished. Herein, we disclose a nickel-catalyzed 1,1-difluoroethylation of arylboronic acids with CH3CF2Cl for the synthesis of (1,1-difluoroethyl)arenes.

SUBMITTER: Liu J 

PROVIDER: S-EPMC9071211 | biostudies-literature | 2019 Sep

REPOSITORIES: biostudies-literature

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1,1-Difluoroethyl chloride (CH<sub>3</sub>CF<sub>2</sub>Cl), a novel difluoroalkylating reagent for 1,1-difluoroethylation of arylboronic acids.

Liu Jianchang J   Zhang Jida J   Wu Chaolin C   Liu Hefu H   Liu Hui H   Sun Fenggang F   Li Yueyun Y   Liu Yuying Y   Dong Yunhui Y   Li Xinjin X  

RSC advances 20190909 49


1,1-Difluoroethylated aromatics are of great importance in medicinal chemistry and related fields. 1,1-Difluoroethyl chloride (CH<sub>3</sub>CF<sub>2</sub>Cl), a cheap and abundant industrial raw material, is viewed as an ideal 1,1-difluoroethylating reagent, but the direct introduction of the difluoroethyl (CF<sub>2</sub>CH<sub>3</sub>) group onto aromatic rings using CH<sub>3</sub>CF<sub>2</sub>Cl has not been successfully accomplished. Herein, we disclose a nickel-catalyzed 1,1-difluoroethyla  ...[more]

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