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Significance: Chiral pyridone backbones can be found in many bioactive compounds. The authors have developed a nickel-catalyzed enantioselective C–H functionalization of 2and 4-pyridones by using a bulky N-heterocyclic ligand. Comment: This nickel-catalyzed reaction permits the enantioselective intramolecular C–H functionalization of 2and 4-pyridones. The nickel complex, based on a chiral bulky N-heterocyclic ligand, is effective in terms of selectivity, giving chiral 2and 4-pyridones in good yields and with high enantioselectivities. Selected examples: X N O R1 R2 Ni(cod)2 (10 mol%) ligand (11 mol%) MAD (40 mol%)

Nickel-Catalyzed Asymmetric C–H Functionalization of Pyridones