2-(1-methyl-pyrrolidin-3-yl)-2,2-diphenyl-acetamide | 3192-68-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-(1-methyl-pyrrolidin-3-yl)-2,2-diphenyl-acetamide
• 英文别名: α,α-diphenyl-α-(1-methyl-3-pyrrolidinyl)acetamide；2-(1-Methylpyrrolidin-3-yl)-2,2-diphenylacetamide
• CAS: 3192-68-5
• 化学式: C₁₉H₂₂N₂O
• 分子量: 294.396
• InChiKey: CMUUWWNPFBUXGO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  22
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  46.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-(1-methyl-pyrrolidin-3-yl)-2,2-diphenyl-acetamide 在 溴 、 sodium methylate 作用下， 以 甲醇 、 硫酸 为溶剂， 生成 1-Methyl-3-diphenylmethylen-pyrrolidin
  参考文献：
  名称：

  Production of methylene-cycloamines

  摘要：

  本发明提供了一种改进的方法来生产亚甲基环氨基化合物，例如1-异丙基-3-二苯基亚甲基乙炔：##STR1## 根据本发明的方法，上述示例的亚甲基氮杂环化合物通过以下步骤合成：(1)将.alpha.,.alpha.-二苯基-.alpha.-(1-异丙基-3-氮杂环基)乙酰胺与溴和碱金属醇盐在改良的霍夫曼重排反应条件下反应，形成一种氨基甲酸酯中间体，(2)在酸性介质中加热氨基甲酸酯中间体，得到1-异丙基-3-二苯基亚甲基氮杂环产物。这种3-亚甲基氮杂环化合物具有一系列药理特性，表明它作为一种情绪提升的治疗剂对于缓解人类的抑郁症状具有实用性。

  公开号：

  US04242261A1

文献信息

• Quaternary ammonium diphenylmethyl compounds useful as muscarinic receptor antagonists
  申请人：Ji YuHua

  公开号：US20080207736A1

  公开（公告）日：2008-08-28

  The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R 1-6 , a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.

  该发明提供了以下公式I的化合物：以盐或带电中性形式或其药用可接受的盐形式存在，其中R1-6，a-e和Q的定义如规范中所述。这些化合物是肌肉萎缩受体拮抗剂。该发明还提供了含有这些化合物的药物组合物，制备这些化合物的方法以及使用这些化合物的方法，例如，用于治疗慢性阻塞性肺疾病和哮喘等肺部疾病。
• Substituted pyrrolidine and related compounds
  申请人：Mammen Mathai

  公开号：US20070078163A1

  公开（公告）日：2007-04-05

  This invention is directed to compounds of formula I: wherein R 1 -R 5 and a-e are as defined in the specification; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof. The invention also directed to pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors using such compounds.

  本发明涉及式I的化合物：其中R1-R5和a-e如规范中所定义；或其药学上可接受的盐、溶剂或立体异构体。本发明还涉及含有这些化合物的药物组合物；用于制备这些化合物的有用中间体和过程；以及使用这些化合物治疗由毒蕈碱受体介导的疾病状况的方法。
• Substituted 4-amino-benzylpiperidine compounds
  申请人：Mammen Mathai

  公开号：US20090023777A1

  公开（公告）日：2009-01-22

  This invention provides 4-amino-1-benzylpiperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome, asthma and chronic obstructive pulmonary disease, using such compounds.

  本发明提供4-氨基-1-苄基哌啶及其相关化合物和药学上可接受的盐，其作为毒蕈碱受体拮抗剂具有用途。本发明还提供含有这些化合物的制药组合物；用于制备这些化合物的有用中间体和过程；以及使用这些化合物治疗由毒蕈碱受体介导的疾病情况，例如过度活跃的膀胱、肠易激综合征、哮喘和慢性阻塞性肺疾病等的方法。
• Substituted 4-amino-1-(pyridylmethyl)piperidine and related compounds
  申请人：Mammen Mathai

  公开号：US20080091034A1

  公开（公告）日：2008-04-17

  This invention provides 4-amino-1-(pyridylmethyl)piperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome and chronic obstructive pulmonary disease, using such compounds.

  本发明提供了4-氨基-1-(吡啶甲基)哌啶及其相关化合物和药学上可接受的盐，它们可用作毒蕈碱受体拮抗剂。本发明还提供了含有这些化合物的制药组合物；用于制备这些化合物的有用中间体和过程；以及使用这些化合物治疗由毒蕈碱受体介导的疾病状态，例如过度活跃的膀胱、肠易激综合征和慢性阻塞性肺疾病的方法。
• Muscarinic receptor antagonists
  申请人：Aggen James

  公开号：US20090306134A1

  公开（公告）日：2009-12-10

  Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.

  本发明涉及一种多结合化合物，其为肌动蛋白受体拮抗剂。该发明的多结合化合物包含2至10个配体共价连接到一个或多个连接体上。每个配体是独立的，可以是肌动蛋白受体拮抗剂或变构调节剂，但至少其中一个配体是肌动蛋白受体拮抗剂。本发明的多结合化合物在治疗和预防慢性阻塞性肺疾病、慢性支气管炎、肠易激综合征、尿失禁等疾病方面具有用途。