A process for the preparation of brivaracetam and intermediates thereof

CN115851866BActive Publication Date: 2026-08-28ZHEJIANG APELOA JIAYUAN PHARMA +1
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Patent Information

Application Number
CN202211656940.7
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2022-12-22
Publication Date
2026-08-28
Estimated Expiration
2042-12-22

AI Technical Summary

Technical Problem

[0004]此前报道的布瓦西坦合成路线，有两个十分明显的不足，第一，合成路线长，且复杂，总产率低，如CN108503610A和CN108503609A提到的使用(R)-4-丙基-二氢呋喃-2-酮作为关键中间体，再经过数步反应得到布瓦西坦，该类制备方法，仅中间体的制备便极为复杂

Benefits of technology

[0061]同现有技术相比，本发明的有益效果体现在：本发明使用了全新路线，新路线反应简单易于操作，整个反应路线收率高，成本低，且无须使用手性拆分剂进行手性拆分，光学纯度高，适合工业化生产。

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Abstract

The application discloses a preparation method of brivaracetam, and the brivaracetam is synthesized through four steps from (R)-4-propylpyrrol-2-one and ethyl 2-bromobutyrate as raw materials. The preparation method of the application does not need to use a resolving agent for chiral resolution, and a hydrolytic enzyme is selected to perform stereoselective hydrolysis, so that the method has high yield, simple post-treatment and low cost, and is a process route more suitable for industrial production. The application further discloses a preparation method of a brivaracetam intermediate.
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Citation Information

Patent Citations

  • Optically pure (R)-4-n-propyl-dihydrofuran-2(3H)-one preparation method

    CN108503609A

  • Optically pure (R)-4-n-propyl-dihydrofuran-2(3H)-one preparation method

    CN108503610A

  • Enzymatic process for the preparation of (2S)-2-[(4R)-2-oxo-4-propyl-pyrrolidin-1-yl]butyric acid and its conversion into brivaracetam

    US11400074B1