Synthesis of 3,4,5-trisubstituted piperidine via S_N2’ reaction

Abstract

3,4,5-Trisubstituted piperidine-containing compounds displayed a range of biological activities, are potential drug candidates to treatment of Alzheimer’s disease, sexual dysfunctions or obesity, heart and kidney insufficiency. However, the inherent difficulty in obtaining a variety of 3,4,5-trisubstituted piperidines has greatly hindered their systematic medicinal chemistry studies for them. In this paper, we disclose an efficient synthesis of racemic and chiral 3,4,5-trisubstituted piperidines via S_N2’ reaction.

Graphical Abstract

Keywords:

• 3,4,5-Trisubstituted piperidine
• SN2’ reaction
• synthesis

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

We gratefully acknowledge the financial support from National Natural Science Foundation of China [21372149, 21572125] and the Fundamental Research Funds for the Central Universities of China [GK201703023] and Shaanxi Normal University.