抗癫痫药物奥卡西平的合成  

Synthesis of Antiepileptic Drug Oxcarbazepine

作　　者：胡伟[1] 谢建伟[1] 蒋祖林 许建帼[1] 谢艳[1] 叶冬菊[1] 

机构地区：[1]衢州学院,浙江衢州324000 [2]浙江九洲药业股份有限公司,浙江台州318000

出　　处：《化工生产与技术》2010年第4期35-37,共3页Chemical Production and Technology

基　　金：浙江省教育厅2007高校科研重点项目(20070897);衢州市2005科技计划项目(2005C31036)

摘　　要：以10-甲氧基-5H-二苯并[b,f]氮杂(艹卓)为原料,通过酰氯化、氨解、水解得到抗癫痫药物奥卡西平,总收率达72%左右,纯度大于99%。在10-甲氧基-5H-二苯并[b,f]氮杂(艹卓)酰用量为20 g的情况下,氯化反应的优化条件为:温度105℃,反应时间3.5 h,催化剂用量7.2 g,溶剂甲苯140mL,反应收率在86%左右。应用双(三氯甲基)碳酸酯替代光气,避免了有毒危险性试剂的使用,工艺简洁、操作方便。Synthesis method of oxcarbanzepine(OCBZ) was introduced in this paper.10-methoxy-5H-dibenz(b,f)azepine was used as the starting material,via acylchlorination,ammonolysis and hydrolysis to give OCBZ with the total yield about 72%and purity over 99%.Hydroxyquinoxaline was prepared by reacting phenylenediamine with glyoxylic acid of different grades.The yield is 86%while the optimized conditions were as follows:the temperature of chlorination is 105℃,reaction time is 3.5 h,and the reacting dose of 10-methoxy-5H-dibenz(b,f) azepine,catalyst,toluene are 20 g,7.2 g,140 mL.The above process of initial material of oxcarbazepine was simplified tremendously,thus avoiding the use of a dedicated plant.,which is of great economic and social benefit.

关 键 词：奥卡西平 双(三氯甲基)碳酸酯 10-甲氧基-5H-二苯并[b f]氮杂革 酰氯化 合成 

分 类 号：TQ463.5[化学工程—制药化工]