Highly mono-selective ortho-trifluoromethylation of benzamides via 8-aminoquinoline assisted Cu-promoted C–H activations

Abstract

A highly mono-selective ortho-trifluoromethylation of benzamides was achieved via Cu-promoted C–H activations. The reaction employs an 8-aminoquinoline group as the bidentate directing group and Togni reagent II as the CF₃ source. The reaction tolerated a wide variety of functional groups and various ortho-trifluoromethylated benzamides were efficiently synthesized in 36–82% yield.