Cu-catalyzed direct C1−H difluoromethylation of pyrrolo[1,2-a]quinoxalines

Abstract An efficient Cu-catalyzed direct C1−H difluoromethylation of pyrrolo[1,2-a]quinoxalines with BrCF2CO2Et or BrCF2CONEt2 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.