The stereoselective formation of six-membered nitrogen heterocycles that contain an asymmetric quaternary carbon center was achieved through aza-annulation of β-enamino amide substrates with activated acrylate derivatives. Condensation of a racemic β-keto amide with an optically active primary amine, either (R)-α-methylbenzylamine or α-amino esters, generated the corresponding optically active tetrasubstituted secondary enamine, ...
