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A novel library of amino-substituted 2-pyridones has been constructed through a two-step sequence of microwave-promoted Buchwald-Hartwig amination of 2-benzyloxy halopyridines followed by debenzylation. Microwave-promoted amination of 3- or 4-halopyridine in the presence of a suitable palladium catalyst and ligand system provided amino-substituted 2-benzyloxypyridines in excellent yields. Then, debenzylation of 2- benzyloxypyridines afforded the corresponding 2-pyridones with high efficiency.

A General Strategy for the Synthesis of Amino-Substituted 2-Pyridones Using a Palladium-Catalyzed Amination Reaction