有机化学 ›› 2006, Vol. 26 ›› Issue (03): 354-356. 上一篇    下一篇

研究简报

Beckmann重排法合成抗癫痫药加巴喷丁

徐显秀,魏忠林,柏旭*   

  1. (吉林大学组合化学研究中心 长春 130012)
  • 收稿日期:2005-01-05 修回日期:2005-09-05 发布日期:2006-02-28
  • 通讯作者: 柏旭

Beckmann Rearrangement as a Key to Gabapentin

XU Xian-Xiu,WEI Zhong-Lin,BAI Xu*   

  1. (Center for Combinatorial Chemistry and Drug Discovery, Jilin University, Changchun 130012)
  • Received:2005-01-05 Revised:2005-09-05 Published:2006-02-28
  • Contact: BAI Xu

由亚甲基环己烷出发, 采用[2+2]环加成和Beckmann重排策略, 经四步反应在比较温和的条件下合成了抗癫痫药物加巴喷丁盐酸盐.

关键词: [2+2]环加成, Beckmann重排, 加巴喷丁, 抗癫痫

Gabapentin, an anticonvulsant agent, was synthesized via [2+2] cycloaddition reaction of methylenecyclohexane with dichloroketene, followed by Beckmann rearrangement of spiro[3,5]nonan-2-one.

Key words: Beckmann rearrangement, anticonvulsant, gabapentin, [2+2] cycloaddition