Chinese Journal of Applied Chemistry

• Full Papers • Previous Articles     Next Articles

Synthesis of Piperidine Derivatives from 1,5-Diols

JAING Fuxiang1, LIU Qiaozhen1, WANG Guo1, CHEN Heru1,2*   

  1. (1.Institute of Traditional Chinese Medicine & Natural Products,College of Pharmacy;
    2.Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and
    New Drugs Research,Jinan University,Guangzhou 510632,China)
  • Received:2012-11-12 Revised:2013-03-22 Published:2013-07-10 Online:2013-07-10
  • Contact: Chen He-Ru

Abstract: A series of piperidine derivatives was synthesized using 1,5-diols as starting materials. The procedures include the sulfonylation of 1,5-diols to active 1,5-disulfonates followed by the cyclization of the 1,5-disulfonates with primary amines. The effects of reaction temperature, time on the annulation were further explored. It was disclosed that when the solvent was primary amine, reaction temperature was 90~100 ℃, and reaction time was 18 h, the yields of 74%~94% for annulations could be reached.

Key words: diols, piperidine, iminosugar, Organic Synthesis

CLC Number: