(R)-4-Methyl-7-trifluoromethyl-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole | 396074-54-7

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: (R)-4-Methyl-7-trifluoromethyl-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole
• 英文别名: (4R)-4-methyl-7-(trifluoromethyl)-1,2,3,4-tetrahydropyrazino[1,2-a]indole
• CAS: 396074-54-7
• 化学式: C₁₃H₁₃F₃N₂
• 分子量: 254.255
• InChiKey: BJUXLBXNDSQYLT-MRVPVSSYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  18
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  17
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (R)-4-Methyl-7-trifluoromethyl-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole 在 sodium borohydrid 作用下， 以 四氢呋喃 、 三氟乙酸 为溶剂， 生成 (4R,10AR)-4-methyl-7-trifluoromethyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indole hydrochloride
  参考文献：
  名称：

  Anti-obesity 1,2,3,4,10,10-a-hexahydropy razino [1,2-a] indoles

  摘要：

  本发明涉及1,2,3,4,10,10a,-六氢吡唑[1,2-a]吲哚衍生物以及药用可接受的盐、溶剂合物和酯，其中R1至R8具有如权利要求1中所述的意义，用于以药物制剂的形式治疗或预防中枢神经系统疾病、中枢神经系统损伤、心血管疾病、胃肠疾病、尿崩症、肥胖和睡眠呼吸暂停。

  公开号：

  US20020035110A1
• 作为产物：
  描述：

  1-((R)-2-tert-Butoxycarbonylamino-1-methyl-ethyl)-6-trifluoromethyl-1H-indole-2-carboxylic acid ethyl ester 在 lithium aluminium tetrahydride 、 potassium carbonate 、 三氟乙酸 作用下， 以 甲醇 、 乙醚 、 二氯甲烷 为溶剂， 生成 (R)-4-Methyl-7-trifluoromethyl-1,2,3,4-tetrahydro-pyrazino[1,2-a]indole
  参考文献：
  名称：

  Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists

  摘要：

  Synthesis and evaluation of the activity of new 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists are described. Appropriately substituted, several analogs displayed selectivity against the other 5-HT2 receptor subtypes of I order of magnitude or more. Selectivity was improved for several compounds versus the lead 1, increasing the therapeutic interest in this series of 5-HT2C receptor agonists. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2005.05.074

文献信息

• Piperazine derivatives
  申请人：——

  公开号：US20020169163A1

  公开（公告）日：2002-11-14

  Piperazine derivatives, as well as pharmaceutically acceptable salts, solvates and esters thereof, can be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, type II diabetes, obesity and sleep apnoea.

  哌嗪衍生物以及其中医药可接受的盐、溶剂合物和酯，可用于制药制剂的形式，用于治疗或预防中枢神经系统疾病、中枢神经系统损伤、心血管疾病、胃肠疾病、尿崩症、2型糖尿病、肥胖和睡眠呼吸暂停。
• [EN] PIPERAZINE DERIVATIVES<br/>[FR] DERIVES DE LA PIPERAZINE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2002010169A1

  公开（公告）日：2002-02-07

  The present invention refers to chemical compounds of formula (I) as well as pharmaceutically usable salts, solvates and esters thereof, wherein R1 to R8 have the significance given in claim 1. They can be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, obesity and sleep apnoea.

  本发明涉及化学式（I）的化合物，以及其可用于制药的盐，溶剂合物和酯，其中R1至R8具有权利要求1中给出的意义。它们可以用于制药制剂的形式，用于治疗或预防中枢神经系统的疾病，中枢神经系统的损伤，心血管疾病，胃肠疾病，尿崩症，肥胖症和睡眠呼吸暂停。
• Anti-obesity 1,2,3,4,10,10a-hexahydropyrazino[1,2-a] indoles
  申请人：Bentley Mark Jonathan

  公开号：US20050239789A1

  公开（公告）日：2005-10-27

  The present invention is directed to 1,2,3,4,10,10a,-hexahydropyrazino[1,2-a]indole derivatives as well as pharmaceutically acceptable salts, solvates and esters thereof, wherein R 1 to R 8 have the significance given in claim 1 be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, obesity and sleep apnea.

  本发明涉及1,2,3,4,10,10a,-六氢吡嗪并[1,2-a]吲哚衍生物，以及其药学上可接受的盐、溶剂和酯，其中R1至R8在权利要求书中所给出的意义下使用，用于制备药物制剂，用于治疗或预防中枢神经系统疾病、中枢神经系统损伤、心血管疾病、胃肠道疾病、尿崩症、肥胖症和睡眠呼吸暂停。
• Anti-obesity 1, 2, 3, 4, 10, 10a-hexahydropyrazino[1, 2-a] indoles
  申请人：——

  公开号：US20030216401A1

  公开（公告）日：2003-11-20

  The present invention is directed to 1,2,3,4,10,10a,-hexahydro-pyrazino[1,2-a]indole derivatives as well as pharmaceutically acceptable salts, solvates and esters thereof, wherein R 1 to R 8 have the significance given in claim 1 be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, obesity and sleep apnea.

  本发明涉及1,2,3,4,10,10a,-六氢吡嗪[1,2-a]吲哚衍生物以及药学上可接受的盐、溶剂和酯，其中R1到R8具有权利要求1中所给定的含义，以药物制剂的形式用于治疗或预防中枢神经系统疾病、中枢神经系统损伤、心血管疾病、胃肠道疾病、尿崩症、肥胖症和睡眠呼吸暂停。
• Anti-obesity 1,2,3,4,10,10a-hexahydropyrazino [1,2-a] indoles
  申请人：Bentley Mark Jonathan

  公开号：US20070106076A1

  公开（公告）日：2007-05-10

  The present invention is directed to 1,2,3,4,10,10a,-hexahydropyrazino[1,2-a] indole derivatives as well as pharmaceutically acceptable salts, solvates and esters thereof, wherein R 1 to R 8 have the significance given in claim 1 be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, obesity and sleep apnea.

  本发明涉及1,2,3,4,10,10a,-六氢吡嗪并[1,2-a]吲哚衍生物以及其药学上可接受的盐、溶剂和酯，其中R1至R8具有权利要求1中所给出的意义，可用于制成药物制剂，用于治疗或预防中枢神经系统疾病、中枢神经系统损伤、心血管疾病、胃肠道疾病、尿崩症、肥胖症和睡眠呼吸暂停。