Synthesis of cis‐3‐methyl‐4‐aminopiperidine Derivatives

Abstract

A facile approach for the preparation of cis‐3‐methyl‐4‐aminopiperidine derivatives is described. The synthesis was carried out via regioselective ring opening of N‐benzyl‐3‐methyl‐3,4‐epoxi‐piperidine (8), which can be easily obtained in two steps from the corresponding N‐benzyl‐pyridinium salt (5). Seven new cis‐3‐methyl‐4‐amino and amido piperidines compounds were obtained.

Keywords:

• 3,4‐Disubstituted piperidine
• epoxide
• pyridinium salt

Acknowledgments

The authors thank Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq) for the fellowships to F. F. H. and D. C. S.