Oxidant- and Base-Free, Copper-Catalyzed Difluoromethylation of Haloalkynes

We report herein a highly efficient copper-catalyzed protocol for the transformation of haloalkynes to the corresponding difluoromethylated alkynes. This scalable protocol exhibits a broad substrate scope and excellent functional group tolerance, enabling the late-stage difluoromethylation of bioactive molecules. Additionally, the strategy of utilizing the difluoromethylalkynes in gram-scale reactions and multiple transformations has proven to be highly valuable in synthetic chemistry.