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A kind of intermediate compound for preparing buvaracetam and its preparation method and application

A technology for compounds and intermediates, applied in the field of drug synthesis, can solve the problems of inapplicability to large-scale production, high cost, and difficulty in purification.

Active Publication Date: 2022-01-04
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, 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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  • A kind of intermediate compound for preparing buvaracetam and its preparation method and application
  • A kind of intermediate compound for preparing buvaracetam and its preparation method and application
  • A kind of intermediate compound for preparing buvaracetam and its preparation method and application

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[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 present invention provides an intermediate for preparing buvaracetam and its preparation method and use, including intermediate compound A, intermediate compound B and its preparation method, and the synthesis of brivaracetam by using intermediate compound B route. In the technical scheme provided by the present invention, high-quality and high-optical-purity buvaracetam and its intermediates can be obtained. Among the four optical isomers, the proportion of brivaracetam is greater than 99.5%; and there is no need to use silica gel column separation and purification , and there is no need to use expensive chiral high-performance liquid phase separation, which avoids cumbersome separation and purification steps, avoids waste of raw materials, reduces production costs, and is more suitable for 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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Patent Type & Authority Patents(China)
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