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以乙酰乙酸乙酯(2)为原料,经溴代得4-溴代-3-氧代丁酸乙酯(4),甘氨酸(3)经酯化反应得甘氨酸甲酯盐酸盐(5)。在碱性条件下,4和5环合生成2-(2,4-二氧代-1-吡咯烷基)乙酸甲酯(6),6经还原、氨化得奥拉西坦(1)粗品,经重结晶后纯度为99.3%,总收率43.4%(以2计)。该路线起始原料易得,反应条件温和,操作简便,成本较低。由4和5合成6的方法未见文献报道。
Glycolic acid methyl ester hydrochloride (5) was obtained by esterification reaction of ethyl 4-bromo-3-oxobutanoate (4) and glycine (3) with ethyl acetoacetate (2) . Under basic conditions, 4 and 5 are cyclized to produce methyl 2- (2,4-dioxo-1-pyrrolidinyl) acetate (6), which is reduced and aminated to oxiracetam (1) The crude product, after recrystallization purity of 99.3%, the total yield of 43.4% (2 dollars). The route is easy to get the starting materials, mild reaction conditions, easy operation, low cost. The synthesis of 6 from 4 and 5 has not been reported in the literature.