丁酸氯维地平的合成工艺研究  

5-Diester-Dihydropyridine Process of Drugs Synthesis

作　　者：马俊[1] 吴红菱[2] 张围宇[3] 万芬[1] 王红[3] 

机构地区：[1]湖北中医药大学药学院 [2]湖北医药学院药学院,湖北武汉430065 [3]湖北中医药大学,湖北武汉430065

出　　处：《湖北中医药大学学报》2011年第6期46-48,共3页Journal of Hubei University of Chinese Medicine

摘　　要：目的通过对该类化合物合成路线及工艺的探讨,为构建一个工业化生产5-双酯-二氢吡啶类药物研究和开发平台提供一定的借鉴和参考。方法以双乙烯酮为原料,与羟基腈类化合物和醋酸铵反应得氨基巴豆酸腈基酯类化合物。再通过Hantzsch缩合,成盐、成酯反应生成目标化合物。结果成功的合成了预期的化合物丁酸氯维地平,总收率达30.6%。结论本实验找到反应条件稳定,后处理简单,大大降低工业成本,易用于工业化生产的合成丁酸氯维地平的生产工艺。Objective Compounds through the process of synthesis routes and to build an industrialized production of 5 - diester - dihy- dropyridine drugs research and development platform. Methods diketene as raw materials, and hydroxy nitriles and ammonium acetate by the reaction of amino- crotonic acid cyano esters,Through Hantzsch Condensation, Salt forming reaction, esterification reaction to Generation the target compounds. Results The successful synthesis of the desired compound clevidipine butyrate, total yield reached 30.6%. Conclusions This experiment found a synthetic route that with stable reaction condition and simplicity that is suitable for mass production which significantly reduces industrial costs, and also makes product purification process simole and easily for industrial.

关 键 词：丁酸氯维地平 高血压 短效钙离子通道阻滞剂 合成 

分 类 号：R944.4[医药卫生—药剂学]