Copper-Catalyzed Aerobic S-Amination of Sulfenamides for the Synthesis of Sulfinamidines.

Abstract

Herein, we present a copper-catalyzed oxidative amination of sulfenamides for the synthesis of sulfinamidines. By the employment of air as the terminal oxidant, a diverse array of secondary and primary amines can be efficiently transformed into their corresponding products. This method is well-suited for last-stage functionalization, and the underlying mechanism has been investigated. The transformation is characterized by exceptional chemoselectivity, mild conditions, facile operation, and broad substrate compatibility, which have significant implications for the fields of pharmaceuticals and organic synthesis.