盐酸阿比朵尔的合成工艺改进的研究  

An Improved Synthesis Method of Arbidl Hydrochloride

作　　者：陈树云 高文 

机构地区：[1]江苏盈科生物制药有限公司,江苏泰州225300

出　　处：《清远职业技术学院学报》2015年第4期76-78,共3页Journal of Qingyuan Polytechnic

摘　　要：目的探讨合成盐酸阿比朵尔合成工艺。方法 5-乙酰氧基-1,2-二甲基吲哚-3-羧酸乙酯为起始原料,经溴化反应、与苯硫芬缩合,同时水解、再经胺甲基化、成盐得到盐酸阿比朵尔,并对原合成工艺进行了改进。结果目标化合物的总收率为12.6%,结构经质谱、核磁共振氢谱及元素分析等确证,纯度可达99%,结论本路线反应条件温和,原料来源方便,成本低,产品性状好,收率高,适合规模化的推广生产。Objective： To synthesize Arbidl Hydrochloride. Methods： The synthesis started from commercially available of 5-acetoxy-1, 2- dimethylindole-3- carboxylate by a sequence of reactions including bromination reaction, condensating with thiophenol and hydrolysis reaction, methylating by dimethylamine, salt formation with hydrochloric acid. Results： The final product was fully characterized by HPLC-MS, 1HNMR, element analysis, IR, UV and DTA. The overall yield was 12.6% in hundreds grams scale. Conclusion： This approach is more applicable for industrial production compared with the reported method.

关 键 词：阿比朵尔 制备 化学合成 

分 类 号：R945[医药卫生—微生物与生化药学]