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.
出处
《河北工业科技》
CAS
2013年第3期212-214,共3页
Hebei Journal of Industrial Science and Technology
关键词
奥拉西坦
甘氨酰胺盐酸盐
乙醇
脱保护
还原
oxiracetam
glycinamide hydrochloride
ethanol
deprotection
hydrogenation
