P(NMe₂)₃-Mediated Regioselective N-Alkylation of 2-Pyridones via Direct Deoxygenation of -Keto Esters

A practical and regioselective direct N-alkylation of 2-pyridones is enabled by use of alpha-keto esters in the P(NMe2)(3)-mediated deoxygenation process. The reaction proceeds under mild conditions to produce N-alkylated 2-pyridones with high selectivity and generality, and the protocol is shown to be applicable for the scale-up synthesis, which makes it promising for practical applications.