盐酸普拉克索中间体合成工艺改进  

Improvement of Synthesis Process of Praxol Hydrochloride Intermediate

作　　者：张丽芳[1] 艾丽 姚佳颖[1] 秦旭荣 ZHANG Li-fang;AI li;YAO Jia-ying;QIN Xu-rong(The Biomedical Engineering Center of Hebei Medical University,Shijiazhuang 050011,China)

机构地区：[1]河北医科大学生物医学工程中心,河北石家庄050011

出　　处：《海峡药学》2020年第12期80-82,共3页Strait Pharmaceutical Journal

基　　金：河北省“百人计划”资助项目(No.E2012100008)。

摘　　要：目的提高盐酸普拉克索中间体磺酰化物N-烷基化反应速率。方法采用正丙基溴作为反应的引入剂,四丁基溴化铵作为反应的相转移催化剂;利用正交试验,确定了反应温度、反应时间、正丙基溴和四丁基溴化铵用量四个因素的最佳反应条件。结果与结论此工艺缩短了反应时间,提高了生产效率和终产品的收率,为工业化生产提供依据。OBJECTIVE To increase the reaction rate of N-alkylation of sulfonylate intermediates of pramipexole hydrochloride.MEHTODS N-propyl bromide was used as the introduction agent of the reaction,Tetrabutyl ammonium bromide was used as a phase transfer catalyst.The optimum reaction conditions of reaction temperature,reaction time,amount of N-propyl bromide and tetrabutyl ammonium bromide were determined by orthogonal experiments.RESULTS and CONCLUSION This process shortens the reaction time,increases the production efficiency and the yield of the final product,and provides the basis for industrial production.

关 键 词：盐酸普拉克索 中间体 相转移催化剂 工艺改进 

分 类 号：R917[医药卫生—药物分析学]