Intermediate compounds for preparing brivaracetam, and preparation method and application thereof

Abstract

The invention provides intermediate compounds for preparing brivaracetam, and a preparation method and an application thereof. The invention also provides an intermediate compound A and an intermediate compound B and preparation methods thereof, and a synthetic route for preparing the brivaracetam by adopting the intermediate compound B. According to a technical scheme of the invention, the brivaracetam with high quality and high optical purity and intermediates thereof can be obtained; the ratio of the brivaracetam in four optical isomers is more than 99.5%; a silica gel column is not neededto be used for separation and purification; expensive chiral high-performance liquid chromatography is not needed to be used for resolution; complicated separation and purification steps are avoided;the waste of raw materials is avoided; the cost of production is reduced; and the preparation methods provided by the invention are more applicable to industrial production.

Description

technical field [0001] The invention relates to the field of drug synthesis, in particular to an intermediate compound used for preparing buvaracetam, a preparation method and application thereof. Background technique [0002] The chemical name of Brivaracetam is (S)-2-((R)-2-oxo-4-propylpyrrolidin-1-yl)butanamide, and its structural formula is as follows: [0003] [0004] Brivaracetam is the third-generation anti-epileptic drug newly developed by Belgian pharmaceutical manufacturer UCB. There is a certain inhibitory effect. In 2005, brivaracetam was approved by the FDA and the European Union for the treatment of myoclonic seizures. Currently, a number of phase III clinical trials including adjuvant therapy for partial seizures of epilepsy are underway. Seizures have a good curative effect. The existing synthetic route of buvaracetam and its synthetic method are as follows. [0005] One is Arnaud Schülé (Org.Process Res.Dev.2016,20,1566-1575) who reported the synthes...

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Problems solved by technology

[0011] In view of the above-mentioned shortcoming of the prior art, the object of the present invention is to provide a kind of intermediate compound for preparing buvaracetam and its preparation method and application, for solving the preparation method of buvaracetam in the prior art The reaction conditions in the method are harsh, the cost is high, it is not easy to purify, and it is not suitable for large-scale industrial production.

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