(6R,7R)-7-amino-8,8-diethyl-6-methoxy-5,6,7,8-tetrahydro-naphthalen-2-ol | 1160275-30-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: (6R,7R)-7-amino-8,8-diethyl-6-methoxy-5,6,7,8-tetrahydro-naphthalen-2-ol
• 英文别名: trans-7-Amino-8,8-diethyl-6-methoxy-5,6,7,8-tetrahydro-naphthalen-2-ol；(6R,7R)-7-amino-8,8-diethyl-6-methoxy-6,7-dihydro-5H-naphthalen-2-ol
• CAS: 1160275-30-8
• 化学式: C₁₅H₂₃NO₂
• 分子量: 249.353
• InChiKey: RAIOBZHCWPSYOH-KGLIPLIRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  55.5
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  trans-(1,1-Diethyl-7-hydroxy-3-methoxy-1,2,3,4-tetrahydronaphthalen-2-yl)-carbamic acid tert-butyl ester 、 盐酸 、 1,4-二氧六环 以 二氯甲烷 为溶剂， 反应 16.03h， 以to give the title compound (5.5 g) (m/z)的产率得到(6R,7R)-7-amino-8,8-diethyl-6-methoxy-5,6,7,8-tetrahydro-naphthalen-2-ol
  参考文献：
  名称：

  Amino- and amido-aminotetralin derivatives and related compounds as mu opioid receptor antagonists

  摘要：

  本发明提供式(I)的氨基和酰胺氨基四氢萘化合物，其中R1，R2，R3，R4，R5，R6，R7和n在规范中定义，或其药学上可接受的盐，该化合物是μ阿片受体拮抗剂。本发明还提供包含这种化合物的制药组合物，使用这种化合物治疗与μ阿片受体活性相关的疾病的方法，以及用于制备这种化合物的过程和中间体。

  公开号：

  US08952031B2

文献信息

• AMINO- AND AMIDO-AMINOTETRALIN DERIVATIVES AND RELATED COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS
  申请人：Trapp Sean G.

  公开号：US20090247627A1

  公开（公告）日：2009-10-01

  The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

  这项发明提供了式(I)的氨基和酰胺氨基四氢萘化合物：其中R1、R2、R3、R4、R5、R6、R7和n在说明书中有定义，或其药用盐，它们是μ阿片受体拮抗剂。该发明还提供了包含这些化合物的药物组合物，使用这些化合物治疗与μ阿片受体活性相关的疾病的方法，以及用于制备这些化合物的过程和中间体。
• AMINOTETRALIN COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS
  申请人：Leadbetter Michael R.

  公开号：US20090149465A1

  公开（公告）日：2009-06-11

  The invention provides aminotetralin compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , n, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

  该发明提供了公式（I）的氨基四氯化合物：其中R1、R2、R3、R4、R5、R6、R7、n和m在规范中定义，或其药用可接受盐，这些化合物是μ阿片受体的拮抗剂。该发明还提供了包含这种化合物的药物组合物，使用这种化合物治疗与μ阿片受体活性相关的疾病的方法，以及用于制备这种化合物的过程和中间体。
• 3-CARBOXYPROPYL-AMINOTETRALIN DERIVATIVES AND RELATED COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS
  申请人：Trapp Sean G.

  公开号：US20090149535A1

  公开（公告）日：2009-06-11

  The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

  这项发明提供了式(I)的3-羧基丙基-氨基四氢萘化合物：其中R1、R2、R3、R4、R5和R6在规范中定义，或其药用盐，这些化合物是μ阿片受体拮抗剂。该发明还提供了包含这类化合物的药物组合物，使用这类化合物治疗与μ阿片受体活性相关的疾病的方法，以及用于制备这类化合物的工艺和中间体。
• Aminotetralin compounds as mu opioid receptor antagonists
  申请人：Theravance, Inc.

  公开号：US08101791B2

  公开（公告）日：2012-01-24

  The invention provides aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, n, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

  本发明提供式(I)的氨基四氢萘化合物：其中R1、R2、R3、R4、R5、R6、R7、n和m在说明书中有定义，或其药学上可接受的盐，它们是μ阿片受体拮抗剂。本发明还提供包括这样的化合物的制药组合物，使用这样的化合物治疗与μ阿片受体活性相关的疾病的方法，以及用于制备这样的化合物的过程和中间体。
• 3-carboxypropyl-aminotetralin derivatives and related compounds as mu opioid receptor antagonists
  申请人：Theravance, Inc.

  公开号：US08106232B2

  公开（公告）日：2012-01-31

  The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

  本发明提供了式(I)的3-羧基丙基-氨基四氢萘化合物：其中R1、R2、R3、R4、R5和R6在说明书中定义，或其药学上可接受的盐，这些化合物是μ阿片受体拮抗剂。本发明还提供包括此类化合物的制药组合物，使用这种化合物治疗与μ阿片受体活性相关的病症的方法，以及用于制备这种化合物的过程和中间体。