由1,5-二羟基多羟基烃合成哌啶衍生物  

Synthesis of Piperidine Derivatives from 1,5-Diols

作　　者：江富祥[1] 刘巧珍[1] 王果[1] 陈河如[1,2] 

机构地区：[1]暨南大学药学院中药及天然药物研究所,广州510632 [2]暨南大学广东省中药药效物质基础及创新药物研究重点实验室,广州510632

出　　处：《应用化学》2013年第7期769-775,共7页Chinese Journal of Applied Chemistry

基　　金：国家自然科学基金资助项目(81172982);广东省科技计划项目(2010A030100006)

摘　　要：以1,5-二羟基多羟基烃为原料,通过磺酰化转化为活泼的1,5-二磺酸酯,再与不同类型的伯胺化合物反应生成多羟基哌啶衍生物。探讨了反应温度、反应时间和伯胺类型等条件对成环反应的影响,当反应温度为90～100℃、反应时间为18 h时,成环反应的收率达到了74%～94%。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.

关 键 词：二羟基多羟基烃 哌啶 多羟基哌啶 有机合成 

分 类 号：O629.7[理学—有机化学]