Pd-Catalyzed regio- and enantioselective allylic substitution with 2-pyridones

An efficient method for the asymmetric synthesis of N-substituted 2-pyridones via Pd-catalyzed regio- and enantioselective allylic substitution of hydroxyl-containing allylic carbonates with 2-pyridones has been developed. By using a palladium complex in situ generated from Pd2(dba)3•CHCl3 and phosphoramidite L2 as a ligand, the process allowed rapid access to N- substituted 2-pyridones with complete chemo- and regioselectivities and good to high enantioselectivities.