A convenient and practical method for the preparation of chiral 4-aryl-2-piperidinone from 3- arylglutaric anhydride and (S)-methylbenzylamine is described. Acylation or alkylation at the α-carbon of the chiral 4-aryl-2-piperidinone product afforded chiral trans-3, 4-disubstituted 2- piperidinone derivatives and reduction of the chiral 2-piperidinones with lithium aluminum hydride provided the corresponding enantiomerically pure trans-3, 4-disubstituted ...