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

A technology for compounds and intermediates, applied in the field of pharmaceutical synthesis, can solve the problems of high cost, difficult purification, harsh reaction conditions, etc., and achieve the effects of avoiding waste, reducing production costs, and avoiding separation and purification steps.

Active Publication Date: 2018-12-04
SHANGHAI BOC CHEM CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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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...

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

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Embodiment Construction

[0061] Embodiments of the present invention are described below through specific examples, and those skilled in the art can easily understand other advantages and effects of the present invention from the content disclosed in this specification. The present invention can also be implemented or applied through other different specific implementation modes, and various modifications or changes can be made to the details in this specification based on different viewpoints and applications without departing from the spirit of the present invention.

[0062] It should be noted that the process equipment or devices not specifically indicated in the following examples all adopt conventional equipment or devices in the art.

[0063] In addition, it should be understood that one or more method steps mentioned in the present invention do not exclude that there may be other method steps before and after the combined steps or other method steps may be inserted between these explicitly ment...

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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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Application Information

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IPC IPC(8): C07D307/33C07D207/06
CPCC07D207/06C07D307/33C07B2200/07C07D207/267B01J23/72B01J27/128B01J27/055B01J27/26
Inventor 李尚立郭伟景海林
Owner SHANGHAI BOC CHEM CO LTD
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