A dual removable activating group enabled the Povarov reaction of N-arylalanine esters: synthesis of quinoline-4-carboxylate esters.

A dual removable activating group enabled Povarov reaction of N-arylalanine esters was reported. N-Arylalanine ester was utilized as the sole carbon source to generate N-arylimine and its tautomer, enamine, in situ by aerobic oxidation of sp3 C-H bonds, and then the consecutive reaction delivered the desired quinoline-4-carboxylate esters in high yields.