吡拉西坦的合成工艺改进  

Improved synthesis of piracetam

作　　者：郭靖[1] 刘瑶 宋帅[1] 李洪 田瑜[1] 程卯生[1] 赵冬梅[1] 

机构地区：[1]沈阳药科大学基于靶点的药物设计与研究教育部重点实验室,辽宁沈阳110016 [2]东北制药集团股份有限公司,辽宁沈阳110026

出　　处：《中国药物化学杂志》2015年第3期190-193,共4页Chinese Journal of Medicinal Chemistry

摘　　要：目的改进吡拉西坦的合成工艺,以实现工业化生产。方法以α-吡咯烷酮和氯乙酸甲酯为原料,两者反应后不经处理直接氨解,即可制备吡拉西坦,再经重结晶得到精品吡拉西坦。结果与结论目标化合物的结构经质谱、核磁共振氢谱、碳谱确证,总收率为73.6%(以α-吡咯烷酮计),纯度大于99.9%。新工艺路线改进了氨化反应条件和重结晶条件,操作简单、收率提高、条件温和,已实现工业化生产。Piraceatm, which chemical name is 2-（ 2-oxopyrrolidino ）acetamide, is an important cognition enhancer. The synthetic route of piracetam suitable for industrial manufacturing was optimized in this paper. 2-Pyrrolidone was used as starting materials to give target compound via reaction with methyl chloroacetate, followed by ammonolysis to afford crude piracetam, which was subjected to recrystallization to get refined product. The target compound was characterized by MS, 1H-NMR,13 C-NMR and the total yield was 73.7 % （based on pyrrolidone）. The purity of the refined product was greater than 99.9%. The improved process has several advantages such as mild conditions, higher yields and simple operations. Anyway it＇s more suitable for industrial production.

关 键 词：吡拉西坦 工艺改进 重结晶 

分 类 号：R914[医药卫生—药物化学]