4-{[(1S)-1-(aminocarbonyl)propyl]amino}butanoic acid | 429674-11-3

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 4-{[(1S)-1-(aminocarbonyl)propyl]amino}butanoic acid
• 英文别名: 4-[[(2S)-1-amino-1-oxobutan-2-yl]amino]butanoic acid
• CAS: 429674-11-3
• 化学式: C₈H₁₆N₂O₃
• 分子量: 188.227
• InChiKey: JUODSNRKJOVATP-LURJTMIESA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.8
• 重原子数：
  13
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.75
• 拓扑面积：
  92.4
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• [EN] BRIVARACETAM INTERMEDIATE, PREPARATION METHOD THEREFOR, AND PREPARATION METHOD FOR BRIVARACETAM<br/>[FR] INTERMÉDIAIRE DE BRIVARACÉTAM, SON PROCÉDÉ DE PRÉPARATION, ET PROCÉDÉ DE PRÉPARATION DE BRIVARACÉTAM<br/>[ZH] 一种布瓦西坦中间体、其制备方法及布瓦西坦的制备方法
  申请人：SHANGHAI PUYI CHEMICAL CO LTD

  公开号：WO2019242192A1

  公开（公告）日：2019-12-26

  本发明涉及一种布瓦西坦中间体、其制备方法及布瓦西坦的制备方法。本发明布瓦西坦的制备方法步骤短，原料便宜，简洁高效，不需要柱层析分离异构体或者不对称合成，适合工业化大规模生产。本发明公开了一种如式（II）所示化合物，可以用于布瓦西坦的合成。
• Method for obtaining an antiepileptic agent
  申请人：Surroca Artus Juan Jose

  公开号：US20060142376A1

  公开（公告）日：2006-06-29

  A process for obtaining the pharmaceutical active ingredient, levetiracetam, by means of deaminomethylation of a sufficiently pure enantiomer intermediate (S)-(II), or by means of deaminomethylation of an addition salt thereof with an acid, wherein R 1 and R 2 are either the same or different (C 1 -C 6 )-alkyl radicals, or else R 1 and R 2 together with the nitrogen atom to which they are bonded form a radical selected from the group consisting of 1-pyrrolidinyl, 1-piperidinyl, 1-morpholinyl, 1-piperazinyl and 1-[4-(C 1 -C 4 )-alkylpiperazinyl]. The invention also comprises preparing the sufficiently pure enantiomer intermediate (S)-(II) by treating the corresponding chemically new racemic intermediate (II) with an amine resolving agent, followed by selective crystallisation of a diastereoisomeric salt thereof. It is useful for obtaining levetiracetam on an industrial scale and involves neither hydrogenation nor chromatography.

  一种制备药用活性成分左乙拉西坦的方法，通过对足够纯的对映体中间体(S)-(II)进行脱氨甲基化，或者通过将其与酸形成的加合物进行脱氨甲基化，其中R1和R2可以是相同或不同的(C1-C6)烷基基团，或者R1和R2与它们所结合的氮原子一起形成选择自1-吡咯啉基、1-哌啶基、1-吗啉基、1-哌嗪基和1-[4-(C1-C4)-烷基哌嗪基]的基团。该发明还包括通过使用胺分离剂处理相应的化学新的外消旋中间体(II)，然后选择性结晶其二对映异构体盐制备足够纯的对映体中间体(S)-(II)。该方法在工业规模上用于制备左乙拉西坦，既不涉及氢化也不涉及色谱法。
• N-alkylated gaba compounds, processes for their preparation and their use as medicaments
  申请人：——

  公开号：US20040058991A1

  公开（公告）日：2004-03-25

  The present invention relates to N-alkylated GABA (Gamma-aminobutyric acid) compounds, to processes for their preparation, to their use in therapy and to pharmaceutical compositions containing them. More particularly these compounds are useful for treatment of disorders of the central and/or peripheral nervous system. Of particular interest is their potent anticonvulsant activity.

  本发明涉及N-烷基化GABA（γ-氨基丁酸）化合物，其制备过程，它们在治疗中的应用以及包含它们的药物组合物。更具体地说，这些化合物用于治疗中枢和/或外周神经系统的疾病。特别值得注意的是它们强效的抗惊厥活性。
• BRIVARACETAM INTERMEDIATE, PREPARATION METHOD THEREFOR, AND PREPARATION METHOD FOR BRIVARACETAM
  申请人：Shanghai Puyi Chemical Co., Ltd.

  公开号：EP3812377A1

  公开（公告）日：2021-04-28

  The present invention relates to a brivaracetam intermediate, a preparation method therefor, and a preparation method for brivaracetam. The steps of the method for preparing brivaracetam described in the present invention are short and the raw materials are cheap, moreover, the method is simple and highly effective without requiring isomer separation by means of column chromatography or asymmetric synthesis, being suitable for industrial large-scale production. In addition, disclosed by the present invention is a compound as shown in formula (II), which may be used for the synthesis of brivaracetam.

  本发明涉及一种溴缬氨噻肟中间体、其制备方法以及溴缬氨噻肟的制备方法。本发明所述的双伐巴坦的制备方法步骤短，原料便宜，而且方法简单、高效，不需要柱层析或不对称合成等手段进行异构体分离，适合工业化大规模生产。此外，本发明还公开了一种如式（II）所示的化合物，该化合物可用于合成双伐巴坦。
• Brivaracetam intermediate, preparation method therefor, and preparation method for brivaracetam
  申请人：SHANGHAI PUYI CHEMICAL CO., LTD.

  公开号：US11518741B2

  公开（公告）日：2022-12-06

  The present invention relates to a brivaracetam intermediate, a preparation method therefor, and a preparation method for brivaracetam. The steps of the method for preparing brivaracetam described in the present invention are short and the raw materials are cheap, moreover, the method is simple and highly effective without requiring isomer separation by means of column chromatography or asymmetric synthesis, being suitable for industrial large-scale production. In addition, disclosed by the present invention is a compound as shown in formula (II), which may be used for the synthesis of brivaracetam.

  本发明涉及一种溴缬氨噻肟中间体、其制备方法以及溴缬氨噻肟的制备方法。本发明所述的双伐巴坦的制备方法步骤短，原料便宜，而且方法简单、高效，不需要柱层析或不对称合成等手段进行异构体分离，适合工业化大规模生产。此外，本发明还公开了一种如式（II）所示的化合物，该化合物可用于合成双伐巴坦。