New synthesis method of brivaracetam

A synthesis method and synthetic route technology, applied in the field of drug synthesis, can solve the problems of high cost, low production capacity, and low yield, and achieve the effects of low cost, high production capacity, and high total yield

Inactive Publication Date: 2017-09-29
ASTATECH CHENGDU BIOPHARM CORP
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  • Abstract
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  • Claims
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Problems solved by technology

[0009] The synthesis method mentioned in the patent is cumbersome and needs to be catalyzed by precious metals. The final product needs to be separated by co

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  • New synthesis method of brivaracetam
  • New synthesis method of brivaracetam
  • New synthesis method of brivaracetam

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Embodiment 1

[0057] Embodiment 1 The synthetic method of Bu Waracetam of the present invention

[0058] a. Preparation of Compound C-1

[0059]

[0060]Control the temperature T=0-10°C, add 23.6kg of n-pentanoyl chloride dropwise into the system containing 33kg of S-4-benzyl-2-oxazolidinone, 2.3kg of DMAP, 250kg of DCM, and 28.2kg of triethylamine. After the dropwise addition, the reaction was incubated for 3 hours. After the reaction of raw material B in TLC is completed, 120kg of tap water is added to the reaction solution, washed with water, separated, the water phase is extracted once with 80kg of dichloromethane and treated as waste water, the organic phase is combined, washed once with 120kg of tap water, and then washed with hydrochloric acid water (13kg hydrochloric acid was added into 120kg tap water to prepare) washed once with water, collected the organic phase and washed once with 120kg water again, collected the organic phase. The aqueous phase is treated as wastewater. ...

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Abstract

The invention provides a synthesis method of brivaracetam. The method adopts cheap and easily available pentanoic acid or valeryl halide as an initial raw material, and provides a brand new synthesis route of a brivaracetam medicine, and the whole reaction route has a high total yield. The method has the advantages of high productivity, low cost, and suitableness for large-scale industrial production.

Description

technical field [0001] The invention relates to a method for synthesizing buvaracetam, which belongs to the field of drug synthesis. Background technique [0002] Brivaracetam (brivaracetam) chemical name is (2S)-2-[(4R)-2-oxo-4-propylpyrrolidin-1-yl]butanamide) is the third generation developed by Belgium UCB Antiepileptic drugs, which are structural derivatives of levetiracetam. [0003] Its published three synthesis patents are as follows: [0004] [0005] In the synthesis method mentioned in the patent, the final product needs to pass through the preparative column to separate the isomers, which has high cost and low production capacity. [0006] [0007] In the synthesis method mentioned in the patent, the two steps of the final product and the intermediate need to separate the isomers through a preparative column, which has high cost and low production capacity. [0008] [0009] The synthesis method mentioned in this patent is cumbersome and needs to be c...

Claims

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Application Information

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IPC IPC(8): C07D207/27
CPCC07D207/27
Inventor 刘兴新吴黎明李仟肖建洋郭鹏
Owner ASTATECH CHENGDU BIOPHARM CORP
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