Novel synthesis process for oxiracetam key intermediate 2-(2,4-dioxopyrrolidine-1-yl)-acetamide

Abstract

The invention provides a novel synthesis process for preparing an oxiracetam key intermediate 2-(2,4-dioxopyrrolidine-1-yl)-acetamide by using 4-halogenated acetoacetic ester and glycinamide hydrochloride as raw materials by virtue of a 'one-pot method'. The novel synthesis process has the advantages of being few in reaction steps, high in yield, cheap and easily available in raw materials, simple in post-treatment, has few waste gas, waste water and waste residues and the like.

Description

technical field [0001] The invention relates to a new preparation method for preparing 2-(2,4-dioxopyrrolidin-1-yl)-acetamide, a key intermediate of oxiracetam. Background technique [0002] Oxiracetam, chemical name: 4-hydroxypyrrolidone-2-acetamide, molecular formula: C 6 h 10 N 2 o 3 , the structure is shown in 1: [0003] [0004] 1 [0005] Oxiracetam is a synthetic cyclic derivative of hydroxyaminobutyric acid (GABOB), also known as Olamide, Oxypyramide, and its trade names are neuromet, Heupan, Jianlangxing, etc. It was synthesized for the first time in 1974 by the company and listed in Italy in 1987. It is one of the drugs approved by the US FDA for the treatment of senile dementia. The synthesis routes reported so far generally have shortcomings such as difficult purification or long synthesis routes. As proposed in Japanese Patent JP62026267, a kind of 3-hydroxy-4-halobutanoic acid ethyl ester and glycinamide is used as raw materials to directly prepare ox...

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Problems solved by technology

[0011] Because the reaction selectivity of each step in this synthetic route is high, and related intermediates can be effectively purified, it is easier to obtain high-purity oxiracetam products, but its intermediate 2-(2,4-dioxopyrrole Alkyl-1-yl)acetamides (see 2 for structure) have long synthetic steps,

[0012] The yield is low, only 35%. At present, there is a lack of an efficient synthetic method for this intermediate, so it is necessary to explore its synthetic method to obtain a method suitable for industrial production and efficient synthesis of this intermediate

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