(2R,4S)-2-Ethyl-1,2,3,4-tetrahydro-N-[5-(4-morpholinyl)-2-pyrimidinyl]-6-(trifluoromethyl)-4-quinolinamine | 952582-12-6

• 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: (2R,4S)-2-Ethyl-1,2,3,4-tetrahydro-N-[5-(4-morpholinyl)-2-pyrimidinyl]-6-(trifluoromethyl)-4-quinolinamine
• 英文别名: (2R,4S)-2-ethyl-N-(5-morpholin-4-ylpyrimidin-2-yl)-6-(trifluoromethyl)-1,2,3,4-tetrahydroquinolin-4-amine
• CAS: 952582-12-6
• 化学式: C₂₀H₂₄F₃N₅O
• 分子量: 407.4
• InChiKey: JSSOVXFSZBNHMP-KDOFPFPSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  29
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  62.3
• 氢给体数：
  2
• 氢受体数：
  9

文献信息

• PROCESS FOR PREPARING TETRAHYDROQUINOLINE DERIVATIVES
  申请人：Okamoto Masaki

  公开号：US20090292125A1

  公开（公告）日：2009-11-26

  The present invention is to provide a process for preparing optically active tetrahydroquinoline derivatives which can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, dyslipidemia and the like, and a process for preparing synthetic intermediates thereof. Specifically, (2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine or a salt thereof is prepared with fewer steps without using an optical resolution, and the optically active tetrahydroquinoline derivatives are obtained from the amine compound.

  本发明提供了一种制备光学活性四氢喹啉衍生物的方法，该方法可用于治疗和/或预防动脉硬化性疾病、血脂异常等疾病，以及其合成中间体的制备方法。具体而言，本发明通过少量步骤制备(2R,4S)-2-乙基-6-三氟甲基-1,2,3,4-四氢喹啉-4-胺或其盐，而不使用光学分辨，并从胺化合物中获得光学活性四氢喹啉衍生物。
• A process for preparing tetrahydroquinoline derivatives
  申请人：Mitsubishi Tanabe Pharma Corporation

  公开号：EP2154132A1

  公开（公告）日：2010-02-17

  The present invention is to provide a process for preparing optically active tetrahydroquinoline derivatives which can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, dyslipidemia and the like, and a process for preparing synthetic intermediates thereof.

  本发明旨在提供一种可用于治疗和/或预防动脉硬化性疾病、血脂异常等疾病的光学活性四氢喹啉衍生物的制备工艺及其合成中间体的制备工艺。
• A PROCESS FOR PREPARING TETRAHYDROQUINOLINE DERIVATIVES
  申请人：Mitsubishi Tanabe Pharma Corporation

  公开号：EP2007728A1

  公开（公告）日：2008-12-31
• US8084611B2
  申请人：——

  公开号：US8084611B2

  公开（公告）日：2011-12-27
• [EN] A PROCESS FOR PREPARING TETRAHYDROQUINOLINE DERIVATIVES<br/>[FR] PROCÉDÉ DE PRÉPARATION DE DÉRIVÉS DE TÉTRAHYDROQUINOLINE
  申请人：TANABE SEIYAKU CO

  公开号：WO2007116922A1

  公开（公告）日：2007-10-18

  [EN] The present invention is to provide a process for preparing optically active tetrahydroquinoline derivatives which can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, dyslipidemia and the like, and a process for preparing synthetic intermediates thereof. Specifically, (2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine or a salt thereof is prepared with fewer steps without using an optical resolution, and the optically active tetrahydroquinoline derivatives are obtained from the amine compound.
  [FR] Cette invention concerne un procédé de préparation de dérivés de tétrahydroquinoline optiquement actifs pouvant servir au traitement et/ou à la prévention de maladies telles que des maladies artériosclérotiques, la dyslipidémie et analogue, ainsi qu'un procédé de préparation d'intermédiaires synthétiques de ces dérivés. De manière plus spécifique, la préparation de (2R,4S)-2-éthyl-6-trifluorométhyl-1,2,3,4-tétrahydroquinolin-4-ylamine ou d'un sel de celle-ci est réalisée en un plus petit nombre d'étapes sans résolution optique et les dérivés de tétrahydroquinoline optiquement actifs sont obtenus à partir du composé amine.