Enantioselective Synthesis of Chiral Sulfinamidines via Asymmetric Amination of Sulfenamides Using a Chiral Phosphoric Acid Catalyst

Despite the significant applications of stereogenic-at-sulfur compounds in pharmaceutical sciences and organic chemistry, efficient methods for precise construction of valuable chiral sulfinamidines remain limited. Herein, we disclosed a chiral phosphoric acid-catalyzed asymmetric strategy for the synthesis of chiral sulfinamidines through the direct amination of sulfenamides. This method demonstrated remarkable substrate scope and excellent yields and stereoselectivities across a diverse array of sulfinamidine compounds. The synthetic utility and practicability of this robust protocol were further highlighted through gram-scale reactions, product derivatization and late-stage functionalization of natural products and drugs.