1-(4-甲氧基苯基)-2-氧代吡咯烷-3-羧酸 | 108541-25-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 中文名称: 1-(4-甲氧基苯基)-2-氧代吡咯烷-3-羧酸
• 英文名称: 1-(4-methoxyphenyl)-2-oxopyrrolidine-3-carboxylic acid
• CAS: 108541-25-9
• 化学式: C₁₂H₁₃NO₄
• mdl: MFCD03932871
• 分子量: 235.24
• InChiKey: AIMIQQQEWMWGNW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.333
• 拓扑面积：
  66.8
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• 海关编码：
  2933790090

反应信息

• 作为反应物：
  描述：

  1-(4-甲氧基苯基)-2-氧代吡咯烷-3-羧酸 、 N,N-二甲基甲酰胺 在 三氯氧磷 作用下， 以 氯仿 为溶剂， 以15%的产率得到1-(p-methoxy-phenyl)-5-chloropyrrole-2,4-dicarbaldehyde
  参考文献：
  名称：

  A novel access to bisformylated pyrroles via decarboxylation of N-aryl-γ-lactam-carboxylic acids under Vilsmeier reaction conditions

  摘要：

  A simple methodology for the conversion of substituted N-aryl-gamma-lactam 2/3-carboxylic acids to substituted N-aryl-diformylated pyrroles has been developed. Several gamma-lactam 2/3-carboxylic acids were subjected to Vilsmeier reagent and substituted diformylated pyrroles are isolated in one-step process. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2009.11.005
• 作为产物：
  描述：

  1,1-环丙烷二甲酸环异亚丙酯 、 甲氧苯胺 以 乙腈 为溶剂， 反应 48.5h， 以76%的产率得到1-(4-甲氧基苯基)-2-氧代吡咯烷-3-羧酸
  参考文献：
  名称：

  二螺吲哚-β-内酰胺：通过施陶丁格烯酮亚胺环加成合成和生物学评价

  摘要：

  在这项工作中，我们首次采用一锅施陶丁格烯酮-亚胺环加成优化方法，以 N-芳基-2-氧代-吡咯烷-3-羧酸作为烯酮源合成二螺吲哚-β-内酰胺。二氢吲哚-2-酮与β-内酰胺环的螺结合被认为能够为所得支架提供稳定性和广泛的功能化。获得的二哌氧吲哚在 A549、MCF7、HEK293 和 VA13 细胞系的 MTT 测试中显示出中等细胞毒性，其中一种化合物显示出对大肠杆菌菌株 LPTD 的抗菌活性。

  DOI：

  10.3390/ijms23126666

文献信息

• [EN] INDOLE AMIDE DERIVATIVES AND RELATED COMPOUNDS FOR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES<br/>[FR] DÉRIVÉS D'INDOLAMIDE ET COMPOSÉS ASSOCIÉS DESTINÉS À ÊTRE UTILISÉS DANS LE TRAITEMENT DES MALADIES NEURODÉGÉNÉRATIVES
  申请人：UNIV LEUVEN KATH

  公开号：WO2010142801A1

  公开（公告）日：2010-12-16

  This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.

  本发明提供了新型化合物，以及这些新型化合物作为药物的使用，特别是用于预防或治疗神经退行性疾病，更具体地是一些神经系统疾病，例如统称为tauopathies的疾病，以及以细胞毒性α-突触核蛋白淀粉样蛋白生成为特征的疾病。本发明还涉及将所述新型化合物用于制造用于治疗此类神经退行性疾病的药物。本发明还涉及包括所述新型化合物的药物组合物，以及制备所述新型化合物的方法。
• INDOLE AMIDE DERIVATIVES AND RELATED COMPOUNDS FOR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES
  申请人：Griffioen Gerard

  公开号：US20120083475A1

  公开（公告）日：2012-04-05

  This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.

  该发明提供了新型化合物，以及这些新型化合物用作药物，特别是用于预防或治疗神经退行性疾病，更具体地说是某些神经系统疾病，例如被统称为tau病理学的疾病，以及由细胞毒性α-突触蛋白淀积所特征的疾病。本发明还涉及使用这些新型化合物制备治疗这种神经退行性疾病的药物。本发明还涉及包括这些新型化合物的制药组合物，以及制备这些新型化合物的方法。
• Indole amide derivatives and related compounds for use in the treatment of neurodegenerative diseases
  申请人：Griffioen Gerard

  公开号：US08618138B2

  公开（公告）日：2013-12-31

  This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterized by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.

  本发明提供了新型化合物及其用作药物的新型化合物，更具体地用于预防或治疗神经退行性疾病，更具体地用于某些神经系统疾病，如被称为tau病变的疾病和由细胞毒性α-突触核蛋白淀积引起的疾病。本发明还涉及使用所述新型化合物制备用于治疗此类神经退行性疾病的药物。本发明还涉及包括所述新型化合物的制药组合物以及制备所述新型化合物的方法。
• Indole Amide Derivatives and Related Compounds for Use in the Treatment of Neurodegenerative Diseases
  申请人：Katholieke Universiteit Leuven, K.U. Leuven R&D

  公开号：US20190054068A1

  公开（公告）日：2019-02-21

  This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.
• US8618138B2
  申请人：——

  公开号：US8618138B2

  公开（公告）日：2013-12-31