(2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine | 934274-23-4

• 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-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine
• 英文别名: (2R,4S)-2-ethyl-6-(trifluoromethyl)-1,2,3,4-tetrahydroquinolin-4-amine
• CAS: 934274-23-4
• 化学式: C₁₂H₁₅F₃N₂
• 分子量: 244.26
• InChiKey: HWXJGEDTIYQFAE-SCZZXKLOSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  38
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  (2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine 在 palladium diacetate 、 R-(+)-1,1'-联萘-2,2'-双二苯膦 sodium t-butanolate 作用下， 以 甲苯 为溶剂， 反应 0.75h， 生成 (2R,4S)-4-(5-morpholin-4-yl-pyridin-2-yl-amino)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinoline
  参考文献：
  名称：

  WO2007/116922

  摘要：

  公开号：
• 作为产物：
  描述：

  (2R,4S)-4-amino-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline mesylate 在 sodium t-butanolate 、 水 作用下， 以 甲苯 为溶剂， 反应 2.5h， 生成 (2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine
  参考文献：
  名称：

  WO2007/116922

  摘要：

  公开号：

文献信息

• [EN] PROCESS FOR PREPARING SYNTHETIC INTERMEDIATES FOR PREPARING TETRAHYDROQUINOLINE DERIVATIVES<br/>[FR] PROCÉDÉ DE PRÉPARATION D'INTERMÉDIAIRES SYNTHÉTIQUES POUR LA PRÉPARATION DE DÉRIVÉS DE TÉTRAHYDROQUINOLÉINE
  申请人：DEZIMA PHARMA B V

  公开号：WO2016024858A1

  公开（公告）日：2016-02-18

  The present invention relates to a process for the preparation of synthetic intermediates which may be used in the preparation of tetrahydroquinoline derivatives, which derivatives have an inhibitory activity against cholesteryl transfer protein (CETP), show effects of increasing HDL cholesterol level and decreasing LDL cholesterol level, and can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, hyperlipidemia, dyslipidemia and the like.

  本发明涉及一种用于合成中间体的制备方法，这些中间体可用于合成四氢喹啉衍生物，这些衍生物对胆固醇转运蛋白（CETP）具有抑制活性，表现出增加HDL胆固醇水平和降低LDL胆固醇水平的效果，并可用于治疗和/或预防动脉粥样硬化疾病、高脂血症、血脂异常等疾病。
• 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。
• Process for preparing tetrahydroquinoline derivatives
  申请人：Mitsubishi Tanabe Pharma Corporation

  公开号：US08084611B2

  公开（公告）日：2011-12-27

  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，以及制备其合成中间体的方法。具体而言，本发明通过较少的步骤而不使用光学分辨法，制备了(2R,4S)-2-乙基-6-三氟甲基-1,2,3,4-四氢喹啉-4-基胺或其盐，并从胺化合物中获得了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。
• Process for preparing synthetic intermediates for preparing tetrahydroquinoline derivatives
  申请人：DEZIMA PHARMA B.V.

  公开号：US10112904B2

  公开（公告）日：2018-10-30

  The present invention relates to a process for the preparation of synthetic intermediates which may be used in the preparation of tetrahydroquinoline derivatives, which derivatives have an inhibitory activity against cholesteryl transfer protein (CETP), show effects of increasing HDL cholesterol level and decreasing LDL cholesterol level, and can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, hyperlipidemia, dyslipidemia and the like.

  本发明涉及一种可用于制备四氢喹啉衍生物的合成中间体的制备工艺，该衍生物对胆固醇转移蛋白（CETP）具有抑制活性，具有提高高密度脂蛋白胆固醇水平和降低低密度脂蛋白胆固醇水平的作用，可用于治疗和/或预防动脉硬化性疾病、高脂血症、血脂异常等疾病。