Abstract

• Cu-catalyzed direct C1−H difluoromethylation of pyrrolo[1,2-a]quinoxalines with BrCF 2 CO 2 Et or BrCF 2 CONEt 2 is described. • A series of difluoromethylated pyrrolo[1,2-a]quinoxalines were obtained with good yields. • The method is characterized by good functional group tolerance, broad substrate scope as well as gram-scale synthesis. An efficient Cu-catalyzed direct C1−H difluoromethylation of pyrrolo[1,2- a ]quinoxalines with BrCF 2 CO 2 Et or BrCF 2 CONEt 2 has been reported, providing to a series of difluoromethylated pyrrolo[1,2- a ]quinoxalines with generally good yields. This approach features good compatibility with substituents, broad substrate scope, and gram-scale synthesis. The further transformations of the products are also examined.

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