2,3,4-Trifluoroquinoline

• 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: 2,3,4-Trifluoroquinoline
• 化学式: C₉H₄F₃N
• 分子量: 183.133
• InChiKey: VMRCHEBYEJBVOS-UHFFFAOYSA-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：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  12.9
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  1,1,1,2-四氟乙烷 、 邻氨基三氟甲苯 在 正丁基锂 作用下， 生成 2,3,4-Trifluoroquinoline
  参考文献：
  名称：

  Reactions of trifluorovinyllithium and 1-chloro-2,2-difluorovinyllithium: the synthesis of fluorinated heterocycles

  摘要：

  Trifluorovinyllithium (from 1,1,1,2-tetrafluoroethane [HFC-134a]) reacted with 2-trifluoromethylaniline at -78 degrees C to give 1,2,3-trifluoroquinoline in moderate to good yield. In a similar reaction, 1-chlorodifluorovinyllithium (from 1-chloro-2,2,2-trifluoroethane [HCFC-133a]) yielded 2-chloro-1,3-difluoroquinoline. (C) 1997 Elsevier Science S.A.

  DOI：

  10.1016/s0022-1139(97)00077-8

文献信息

• [EN] QUINOLINE DERIVATIVES AS PDE10A ENZYME INHIBITORS<br/>[FR] DÉRIVÉS DE QUINOLÉINE EN TANT QU'INHIBITEURS D'ENZYME PDE10A
  申请人：LUNDBECK & CO AS H

  公开号：WO2013092974A1

  公开（公告）日：2013-06-27

  The present invention provides quinoline derivatives of formula (I) that are PDE10A enzyme inhibitors, and as such are useful to treat neurodegenerative and psychiatric disorders. Especially, the invention provides compounds that are highly selective for PDE10 over other PDE subtypes. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating disorders using the compounds of the invention.

  本发明提供了公式(I)的喹啉衍生物，它们是PDE10A酶抑制剂，因此可用于治疗神经退行性和精神障碍。特别地，本发明提供了对PDE10比其他PDE亚型高度选择性的化合物。本发明还提供了包含本发明化合物的制药组合物以及使用本发明化合物治疗疾病的方法。
• Quinoline derivatives as PDE10A enzyme inhibitors
  申请人：H. Lundbeck A/S

  公开号：US20150376186A1

  公开（公告）日：2015-12-31

  The present invention provides quinoline derivatives of formula I that are PDE10A enzyme inhibitors, and as such are useful to treat neurodegenerative and psychiatric disorders. Especially, the invention provides compounds that are highly selective for PDE10 over other PDE subtypes. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating disorders using the compounds of the invention.

  本发明提供了式I的喹啉衍生物，它们是PDE10A酶抑制剂，因此可用于治疗神经退行性和精神障碍。特别地，本发明提供了高度选择性作用于PDE10而非其他PDE亚型的化合物。本发明还提供了包含本发明化合物的制药组合物和使用本发明化合物治疗疾病的方法。
• QUINOLINE DERIVATIVES AS PDE10A ENZYME INHIBITORS
  申请人：H. Lundbeck A/S

  公开号：EP2794606A1

  公开（公告）日：2014-10-29
• Quinoline Derivatives as PDE10A Enzyme Inhibitors
  申请人：H. Lundbeck A/S

  公开号：US20160303120A1

  公开（公告）日：2016-10-20

  The present invention provides quinoline derivatives of formula I that are PDE10A enzyme inhibitors, and as such are useful to treat neurodegenerative and psychiatric disorders. Especially, the invention provides compounds that are highly selective for PDE10A over other PDE subtypes. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating disorders using the compounds of the invention.
• US9216986B1
  申请人：——

  公开号：US9216986B1

  公开（公告）日：2015-12-22