CN112955430A - 一种布瓦西坦及其中间体的制备方法 - Google Patents

一种布瓦西坦及其中间体的制备方法 Download PDF

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CN112955430A
CN112955430A CN201980070829.XA CN201980070829A CN112955430A CN 112955430 A CN112955430 A CN 112955430A CN 201980070829 A CN201980070829 A CN 201980070829A CN 112955430 A CN112955430 A CN 112955430A
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brivaracetam
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CN112955430B (zh
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樊海生
占轶鹏
尹凯
季翔
刘丰豪
石凯强
郭效文
黄鲁宁
陶安平
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Shanghai Kesheng Pharmaceutical Research And Development Co ltd
Zhejiang Huahai Pharmaceutical Co Ltd
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Shanghai Kesheng Pharmaceutical Research And Development Co ltd
Zhejiang Huahai Pharmaceutical Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24Oxygen or sulfur atoms
    • C07D207/262-Pyrrolidones
    • C07D207/2632-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/272-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本申请涉及一种布瓦西坦中间体的制备方法(I),包括如下步骤:将B‑P所示化合物和1S,2S‑二苯基乙二胺溶于拆分溶剂中,析晶,过滤,重结晶,得B‑Q所示化合物,再转化为B‑R所示的布瓦西坦中间体;该方法可以有效地拆分B‑P所示化合物。本申请还提供了利用B‑R所示的化合物制备布瓦西坦的方法;该方法在制备过程中不需要采用手性色谱柱分离异构体,仅进行萃取,洗涤,干燥,浓缩等简单步骤即可分离有效成分,分离过程简单,大大降低了布瓦西坦生产成本。
Figure DDA0003039544050000011

Description

PCT国内申请,说明书已公开。

Claims (13)

  1. PCT国内申请,权利要求书已公开。
CN201980070829.XA 2018-12-19 2019-12-12 一种布瓦西坦及其中间体的制备方法 Active CN112955430B (zh)

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CN113651745A (zh) * 2021-09-09 2021-11-16 上海医药工业研究院 布瓦西坦中间体及其制备方法和纯化方法
CN115028563A (zh) * 2022-07-15 2022-09-09 苏州诚和医药化学有限公司 一种布瓦西坦中间体的制备方法

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CN109942516A (zh) * 2019-03-27 2019-06-28 成都克莱蒙医药科技有限公司 化合物ra在制备布瓦西坦中间体手性丁内酯中的用途
CN115806519A (zh) * 2022-12-22 2023-03-17 浙江普洛家园药业有限公司 一种布瓦西坦中间体的拆分方法及其应用

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CN113651745A (zh) * 2021-09-09 2021-11-16 上海医药工业研究院 布瓦西坦中间体及其制备方法和纯化方法
CN115028563A (zh) * 2022-07-15 2022-09-09 苏州诚和医药化学有限公司 一种布瓦西坦中间体的制备方法
CN115028563B (zh) * 2022-07-15 2024-04-09 苏州诚和医药化学有限公司 一种布瓦西坦中间体的制备方法

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US20220048856A1 (en) 2022-02-17
EP3901137B1 (en) 2023-01-25
EP3901137A1 (en) 2021-10-27
EP3901137A4 (en) 2021-11-24

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