Copper-Catalyzed Difluoroalkylative Benzylation of Alkenes

Shulei Ge¹, Xiaonuo Shi¹, Jie Li¹（李杰）*

¹Key Laboratory of Organic Synthesis of Jiangsu Province, College of Chemistry, Chemical Engineering and Materials Science, Soochow University, 215123 Suzhou, China

Org. Lett.2025, 27, 7445

Abstract:A directing-group-free copper-catalyzed difluoroalkylative benzylation of alkenes with difluoroalkyl bromides and benzylzinc pivalates has been disclosed, thus providing a straightforward access to structurally diverse 1,2-diarylalkanes via 2-fold Csp³-Csp³/Csp³-Csp³ bond formation in a regioselective fashion. Moreover, late-stage modifications of various pharmaceutically active molecules should demonstrate the potential utilizations of this method in medicinal chemistry.

Article information: https://doi.org/10.1021/acs.orglett.5c02355