Enantioselective Addition of Azlactones to Ethylene Sulfonyl Fluoride via Dual Catalysis

Enantioselective conjugate addition of azlactones to ethylene sulfonyl fluoride has been achieved via the cooperative catalysis with (DHQD)2PHAL and a hydrogen-bond donor (HBD). This approach furnishes a facile access to a range of structurally diverse azlactone sulfonyl fluoride derivatives with good to excellent yields and enantioselectivities. The combination of azlactone and sulfonyl fluoride group produces valuable unnatural α-quaternary amino acid derivatives for the drug discovery.