Author/Authors :
Schِn، نويسنده , , Uwe and Messinger، نويسنده , , Josef and Buckendahl، نويسنده , , M. and Prabhu، نويسنده , , M.S. and Konda، نويسنده , , A.، نويسنده ,
Abstract :
An efficient Pd(0)-catalyzed protocol for the rapid and efficient preparation of N-aryl and N-heteroaryl substituted piperidones is described. The two step syntheses proceed with an overall yield of 50–70% using X-Phos as optimal ligand for the Pd(0)-catalyzed Buchwald–Hartwig amination followed by subsequent hydrolysis of resulted ketals.
Keywords :
Buchwald–Hartwig amination , PALLADIUM , X-Phos , microwave , 4-Arylpiperidones