A General Method for Site-Selective Csp3-S Bond Formation via Cooperative Catalysis

Herein, we report a copper-catalyzed site-selective thiolation of Csp3-H bonds of aliphatic amine. The method is featured with the broad substrate scope and good functional group compatibility. Both primary, secondary, and tertairy C-H bonds could be converted into C-S bonds with high efficiency. The late-stage modification of biological active compounds by this method was also demonstrated. Furthermore, the one-pot preparation of pyrrolidine or piperidine compounds via a domino process was achieved.