The stereoselective synthesis of 3-substituted and 3,4-disubstituted piperidine and piperidin-2-one derivatives was achieved starting from 2-pyridone. After N-galactosylation and subsequent O-silylation, nucleophilic addition of organometallic reagents proceeded with high regioand stereoselectivity at 4-position. Substituents at position 3 were stereoselectively introduced by reaction of electr...

A mild and efficient Rh(III)-catalyzed regioselective synthesis of isoquinolones and pyridones has been developed. The protocol uses readily available N-methoxybenzamide or N-methoxymethacrylamide and diazo compounds as starting materials. The process involving tandem C-H activation, cyclization, and condensation steps proceeds under mild conditions, and the corresponding isoquinolone and pyrid...