乙酰牛磺酸的合成工艺研究  

Study on the synthesis process of acetyl taurine

作　　者：陈靖赜 张浩 陈凤玲 章文 张志云 王静 CHEN Jing-ze;ZHANG Hao;CHEN Feng-ling;ZHANG Wen;ZHANG Zhi-yun;WANG Jing(Wuhan Jinyintan Hospital,Wuhan 430023,China;Hubei Institute for Drug Control,Wuhan 430064,China)

机构地区：[1]武汉市金银潭医院,湖北武汉430023 [2]湖北省药品监督检验研究院,湖北武汉430064

出　　处：《中国药物化学杂志》2022年第2期102-105,共4页Chinese Journal of Medicinal Chemistry

摘　　要：目的优化乙酰牛磺酸镁关键中间体乙酰牛磺酸的合成工艺。方法乙酰牛磺酸是合成乙酰牛磺酸镁的关键中间体,在文献方法基础上,本文作者设计了以牛磺酸和乙酸酐为原料得到目标化合物乙酰牛磺酸的合成路线,通过ESI-MS、^(1)H、^(13)C-NMR和IR谱对目标化合物的结构进行确证;以收率为指标考察了不同反应温度、反应时间和反应物投料比对目标产物的影响。结果合成乙酰牛磺酸较佳反应条件为乙酸酐和牛磺酸的物质的量比为26∶10,反应温度为140℃,反应时间为30 h,目标化合物的纯度为98.3%,收率为72.9%。结论本合成工艺原料易得、操作简单,目标化合物收率和纯度均较高,对乙酰牛磺酸镁的工业合成具有重要的意义。The synthesis process of acetyl taurine was optimized and the influences of reaction temperature, reaction time and reactants ratio were investigated.The results showed that the optimized conditions were as follows: the molar ratio of acetic anhydride to taurine was 26∶10,the reaction temperature was 140 ℃,and reaction time was 30 h.Under this condition, the yield of product was 72.9% and the purity was 98.3%.The structure of acetyl taurine was confirmed by ESI-MS,^(1)H and ^(13)C-NMR,and IR spectrum.The improved synthetic route has advantages of easy availability of raw materials, simple operation, higher yield and purity, and is of great significance for the industrial application.

关 键 词：乙酰牛磺酸镁 乙酰牛磺酸 合成工艺 收率 

分 类 号：R914[医药卫生—药物化学]