苯乙哌啶合成的改进  

Improved synthesis of diphenoxylate hydrochloride

作　　者：刘宝闫 杏莲胡 海延 

机构地区：[1]开封医学高等专科学校,开封475001

出　　处：《中国现代应用药学》2001年第1期46-47,共2页Chinese Journal of Modern Applied Pharmacy

摘　　要：目的 :改进苯乙哌啶的合成方法 ,使之更适合工业化生产。方法 :以N ,N 双 (β 氯乙基 )对甲苯磺酰胺为原料 ,利用液 液相转移催化方法制得 1 对甲苯磺酰基 4 苯基 4 氰基哌啶 ,再经水解、酯化、缩合、成盐等步骤 ,合成了苯乙哌啶。结果 :总收率可达 5 1.8%。结论 :此合成方法适合工业化生产。OBJECTIVE:Improve the synthetic method of diphenoxylate hydrochloride,which was more suitable for the industrial process.METHOD:N,N bis(β chloroethyl) 4 methyl phenyl sulfonylamine was used as starting material vialiquid liquid phase transfer catalysis to prepare 1 (4 methyl phenyl) sulfonyl 4 phenyl 4 piperidine cabonitrile,which by hydrolysis,esterification,condensation,salifying to yield diphenoxylate hydrochloride.RESULTS:The total yield ammounted to 51.8%.CONCLUSION:The method was suible for the industrial process.

关 键 词：苯乙哌啶 相转移催化 合成 药物中间体 止泻药 

分 类 号：R914.5[医药卫生—药物化学] TQ463.5[医药卫生—药学]