Although bromodifluoromethane （BrCF2H） is a simple and readily available fluorine source, direct formation of difluoromethylated arenes with BrCF2H has not been reported. Herein, we describe an efficient method to a...Although bromodifluoromethane （BrCF2H） is a simple and readily available fluorine source, direct formation of difluoromethylated arenes with BrCF2H has not been reported. Herein, we describe an efficient method to access difluoromethylated arenes through a nickel-catalyzed difluoromethylation of arylboronic acids with BrCF2H. The reaction exhibits high efficiency, good functional group tolerance and broad substrate scope, thus providing an efficient route for applications in drug discovery and development. Preliminary mechanistic studies reveal that a difluoromethyl radical is involved in the reaction.展开更多
Although trifluoromethylthiolated compounds have privileged applications in pharmaceuticals and agrochemicals,efficient strategies for the asymmetric construction of C_(sp)^(3)-SCF_(3)bonds are limited.Specifically,th...Although trifluoromethylthiolated compounds have privileged applications in pharmaceuticals and agrochemicals,efficient strategies for the asymmetric construction of C_(sp)^(3)-SCF_(3)bonds are limited.Specifically,the catalytic asymmetric nucleophilic trifluoromethylthiolation remains challenging.Here,we report a copper-catalyzed enantioselective nucleophilic trifluoromethylthiolation of secondary propargyl sulfonates with trifluoromethylthio silver.The reaction exhibits high efficiency,good enantioselectivity,high functional group tolerance,and broad substrate scope,paving a new way for the asymmetric synthesis of trifluoromethylthiolated compounds.展开更多
基金This work was financially supported by the National Natural Science Foundation of China （Nos. 21425208, 21672238, 21332010, and 21421002）, the Strategic Priority Research Program of Chinese Academy of Sciences （No. XDB20000000）, and SIOC.
文摘Although bromodifluoromethane （BrCF2H） is a simple and readily available fluorine source, direct formation of difluoromethylated arenes with BrCF2H has not been reported. Herein, we describe an efficient method to access difluoromethylated arenes through a nickel-catalyzed difluoromethylation of arylboronic acids with BrCF2H. The reaction exhibits high efficiency, good functional group tolerance and broad substrate scope, thus providing an efficient route for applications in drug discovery and development. Preliminary mechanistic studies reveal that a difluoromethyl radical is involved in the reaction.
基金Financial support for this work was provided by the National Natural Science Foundation of China(nos.21931013,21702225,21672238,and 21421002)the Strategic Priority Research Program of the Chinese Academy of Sciences(no.XDB20000000).
文摘Although trifluoromethylthiolated compounds have privileged applications in pharmaceuticals and agrochemicals,efficient strategies for the asymmetric construction of C_(sp)^(3)-SCF_(3)bonds are limited.Specifically,the catalytic asymmetric nucleophilic trifluoromethylthiolation remains challenging.Here,we report a copper-catalyzed enantioselective nucleophilic trifluoromethylthiolation of secondary propargyl sulfonates with trifluoromethylthio silver.The reaction exhibits high efficiency,good enantioselectivity,high functional group tolerance,and broad substrate scope,paving a new way for the asymmetric synthesis of trifluoromethylthiolated compounds.
