奥拉西坦的合成工艺改进  

Improved synthesis of oxiracetam

作　　者：杨英梅[1] 苏代国[2] 

机构地区：[1]石药集团欧意药业有限公司,河北石家庄050051 [2]河北科技大学体育工作部,河北石家庄050018

出　　处：《河北工业科技》2013年第3期212-214,共3页Hebei Journal of Industrial Science and Technology

摘　　要：介绍了一种合成奥拉西坦的改进方法,以双乙烯酮为起始原料,经氯化开环、酯化得到4-氯-乙酰乙酸甲酯,经氯化、催化甲氧基化两步反应,得到中间产物,再直接与甘氨酰胺盐酸盐在醇类溶剂中环合得到4-甲氧基-吡咯啉-2-酮-1-基乙酰胺,脱甲基保护得到2,4-二氧吡咯啉-1-基乙酰胺盐酸盐,最后还原得到奥拉西坦。该方法简化了操作步骤,总收率达到28.1%,较相关专利提高了5.64%,成本降低,更加适合工业化生产。This article describes an improved method on the synthesis of oxiracetam. There are several steps for the synthesis, first using diketene as the starting material, through chlorination, ring-opening, esterifieation reaction to give 4-chloro-aceto- acetic acid methyl ester, and second using methoxy reaction to directly produce an intermediate product, then it is reacted with glycinamide hydrochloride cyclization in an alcoholic solvent to produce 4- methoxy-pyrrolin-2- one-l-yl-acetamide, and using demethyl to give 2,4-dioxo-pyrrolin-l-yl-acetamide hydrochloride, finally through hydrogenation to give oxiracetam. This ap- proach simplifies the steps, and the total yield reaches 28.1%, 5.64% higher than that of the related patents, while the cost is lower, and it is more suitable for industrial production.

关 键 词：奥拉西坦 甘氨酰胺盐酸盐 乙醇 脱保护 还原 

分 类 号：TQ463.5[化学工程—制药化工]