American Chemical Society
ol3c03198_si_001.pdf (8.97 MB)

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

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journal contribution
posted on 2023-11-03, 18:05 authored by Xujuan Jiang, Yanshan Song, Junjie Peng, Zhiying Zhong, Li Chen, Xiaojun Zeng
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.