奥拉西坦的合成工艺改进

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。

Improved synthesis of oxiracetam

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,esterification reaction to give 4-chloro-acetoacetic 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-1-yl-acetamide,and using demethyl to give 2,4-dioxo-pyrrolin-1-yl-acetamide hydrochloride,finally through hydrogenation to give oxiracetam.This approach 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.