盐酸环苯扎林的合成工艺改进  

Improved synthesis of cyclobenzaprine hydrochloride

作　　者：邢磊[1] 周林波[1] 周启璠 陈国良[1] 

机构地区：[1]沈阳药科大学基于靶点的药物设计与研究教育部重点实验室,辽宁沈阳110016

出　　处：《中国药物化学杂志》2015年第2期115-117,共3页Chinese Journal of Medicinal Chemistry

摘　　要：目的改进盐酸环苯扎林的合成方法。方法以二苯并环庚烯酮为起始原料,与3-(N,N-二甲基氨基)氯丙烷经格氏反应生成5-(3-二甲氨基丙基)-5-羟基二苯并环庚三烯,后经稀盐酸脱水生成环苯扎林,最终与氯化氢乙酸乙酯溶液生成盐酸环苯扎林。结果与结论目标化合物及中间体的结构经1H-NMR、ESI-MS谱等确证,HPLC法检测纯度达99.70%,单个杂质含量小于0.1%。新合成路线操作简便,反应条件温和。使用的原料和试剂成本都比较低廉,总收率为50%,适合工业化生产。Cyclobenzaprine hydrochloride is a muscle relaxant developed by Merck Corp. The synthesis of cyclobenzaprine hydrochloride was improved in this paper. It was synthesized from dibenzo[ a, d] cycloheptene-5-one via Grignard reaction,dehydration and salification with an overall yield of 50%. The structure of target compound was identified by 1H-NMR and ESI-MS. The improved process is facile with relatively convenient operation procedures and suitable for industrial production.

关 键 词：盐酸环苯扎林 合成 工艺改进 

分 类 号：R914.5[医药卫生—药物化学]