One‐Pot Synthesis of Thioamides via Nickel‐Catalyzed Coupling of Thiocarbamoyl Fluorides and Boronic Acids

Abstract A novel and efficient one‐pot method has been developed for the synthesis of thioamides through coupling reactions between thiocarbamoyl fluorides, which are generated in situ from amines, and boronic acids. The key to the success of this transformation lies in the use of nickel a catalyst combined with PCy 3 as a ligand. This innovative reaction protocol provides mild reaction conditions suitable for producing a diverse array of thioamides, and the late‐stage modification of amoxapine was successfully achieved.