α‐Difluoroalkylation of Benzyl Amines with Trifluoromethylarenes

An α‐difluoroalkylation of benzyl amines with trifluoromethylarenes is disclosed herein. This protocol is characterized by its operational simplicity, excellent chemoselectivity and broad scope—even with advanced synthetic intermediates—, thus offering a new entry point to medicinally‐relevant α‐difluoroalkylated amines from simple, yet readily accessible, precursors. A highly modular technique that streamlines the synthesis of α‐difluoroalkylated amines from benzyl amines and trifluoromethylarenes has been developed. This protocol demonstrates remarkable operational simplicity, excellent chemoselectivity, and wide applicability, including with advanced synthetic intermediates, thus providing a novel pathway to access medicinally‐relevant α‐difluoroalkylated amines from readily available and simple precursors.