Tetrahedron letters

An improved synthesis of N-aryl and N-heteroaryl substituted piperidones

…, J Messinger, M Buckendahl, MS Prabhu, A Konda

Index: Schoen, Uwe; Messinger, Josef; Buckendahl; Prabhu; Konda Tetrahedron Letters, 2007 , vol. 48, # 14 p. 2519 - 2525

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Citation Number: 15

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.