N-(2-phenyl-4-quinolinyl)piperazine | 401567-67-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: N-(2-phenyl-4-quinolinyl)piperazine
• 英文别名: 2-Phenyl-4-piperazin-1-ylquinoline
• CAS: 401567-67-7
• 化学式: C₁₉H₁₉N₃
• 分子量: 289.38
• InChiKey: JYAAGAGFNQEOKB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  22
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  28.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-(2-phenyl-4-quinolinyl)piperazine 、 异氰酸乙酯 以 四氢呋喃 为溶剂， 反应 18.0h， 生成 N-ethyl-4-(2-phenyl-4-quinolinyl)-1-piperazinecarboxamide
  参考文献：
  名称：

  Oxadiazoles as bioisosteric transformations of carboxylic functionalities. II

  摘要：

  In order to improve the in vivo efficacy of a series of known benzodiazepine receptor (BZR) ligands, 1-(2-phenyl-4-quinolinyl)-4-piperidinecarboxamides, a series of analogs has been prepared in which the amide group of these ligands has been replaced by a 1,2,4-oxadiazole moiety or converted to other carboxylic isosters such as esters or nitriles. An increase in the in vivo efficacy was observed for some of the compounds prepared in this investigation compared to the parent carboxamide derivatives.

  DOI：

  10.1016/0223-5234(96)89169-0
• 作为产物：
  描述：

  哌嗪 、 4-氯-2-苯基喹啉 以 乙二醇乙醚 为溶剂， 反应 18.0h， 生成 N-(2-phenyl-4-quinolinyl)piperazine
  参考文献：
  名称：

  Oxadiazoles as bioisosteric transformations of carboxylic functionalities. II

  摘要：

  In order to improve the in vivo efficacy of a series of known benzodiazepine receptor (BZR) ligands, 1-(2-phenyl-4-quinolinyl)-4-piperidinecarboxamides, a series of analogs has been prepared in which the amide group of these ligands has been replaced by a 1,2,4-oxadiazole moiety or converted to other carboxylic isosters such as esters or nitriles. An increase in the in vivo efficacy was observed for some of the compounds prepared in this investigation compared to the parent carboxamide derivatives.

  DOI：

  10.1016/0223-5234(96)89169-0

文献信息

• Proline derivatives and use thereof as drugs
  申请人：Kitajima Hiroshi

  公开号：US20050245538A1

  公开（公告）日：2005-11-03

  The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.

  本发明旨在提供具有治疗效果的化合物，其作用是通过DPP-IV的抑制作用，并且作为药物产品具有令人满意的效果。本发明人发现，在丙氨酸的γ位上引入取代基的衍生物具有强效的DPP-IV抑制活性，并通过增加稳定性完成了本发明。
• Proline derivatives and the use thereof as drugs
  申请人：——

  公开号：US20040106655A1

  公开（公告）日：2004-06-03

  The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the &ggr;-position of proline represented by the formula (I) 1 wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.

  本发明旨在提供具有治疗作用的化合物，由于DPP-IV抑制作用而具有满意的药物产品。本发明人发现，具有引入取代基的脯氨酸γ-位置的衍生物，其化学式为(I)1，其中每个符号如规范中所定义，具有强效的DPP-IV抑制活性，并通过增加稳定性完成了本发明。
• PROLINE DERIVATIVES AND USE THEREOF AS DRUGS
  申请人：Mitsubishi Tanabe Pharma Corporation

  公开号：EP1308439B1

  公开（公告）日：2008-10-15
• US7060722B2
  申请人：——

  公开号：US7060722B2

  公开（公告）日：2006-06-13
• US7074794B2
  申请人：——

  公开号：US7074794B2

  公开（公告）日：2006-07-11