Nickel-Catalyzed Hydrotrifluoroalkylation of Alkynes to Construct Allylic Trifluoromethyl Terminal Alkenes

Org Lett. 2023 May 19;25(19):3578-3584. doi: 10.1021/acs.orglett.3c01237. Epub 2023 May 9.

Abstract

Herein, we describe a nickel-catalyzed hydrotrifluoroalkylation of terminal alkyne for the synthesis of a manifold allylic trifluoromethyl terminal alkene. The combination of nitrogen and phosphine ligands, especially electron-rich ones, plays an indispensable role in the course of the reaction, promoting the reactivity to a remarkable level, demonstrating high efficiency, broad substrate scope, and favorable functional group compatibility. The strategy provides a facile method for the synthesis of diversified allylic CF3-containing drugs and bioactive molecules.