Enantioselective Synthesis of N-Cyclopentenyl Sulfoximines via the Catalytic Asymmetric Aza-Piancatelli Reaction

Using sulfoximine as the amine source, a catalytic enantioselective aza-Piancatelli rearrangement of furylcarbinols was developed under chiral Brønsted acid (CBA) catalysis. This method enables the diastereo- and enantioselective synthesis of diverse N-alkyl α-chiral sulfoximines in high yields under mild conditions. Selected derivatizations of the resulting products were conducted to showcase their chemical modifiability.