(R)-2-N,N-Dibenzylamino-5-methoxy-1,2,3,4-tetrahydronaphthalene | 197446-07-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: (R)-2-N,N-Dibenzylamino-5-methoxy-1,2,3,4-tetrahydronaphthalene
• 英文别名: Dibenzyl-((R)-5-methoxy-1,2,3,4-tetrahydro-naphthalen-2-yl)-amine；(2R)-N,N-dibenzyl-5-methoxy-1,2,3,4-tetrahydronaphthalen-2-amine
• CAS: 197446-07-4
• 化学式: C₂₅H₂₇NO
• 分子量: 357.495
• InChiKey: MNNMWEOINNJPCF-HSZRJFAPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.6
• 重原子数：
  27
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  12.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  溴甲苯 、 (R)-5-甲氧基-2-氨基四氢萘 在 potassium carbonate 作用下， 以 乙腈 为溶剂， 生成 (R)-2-N,N-Dibenzylamino-5-methoxy-1,2,3,4-tetrahydronaphthalene
  参考文献：
  名称：

  Derivatives of (R)-2-amino-5-methoxytetralin: Antagonists and inverse agonists at the dopamine D2a receptor

  摘要：

  A series of N-arylmethyl substituted (R)-5-methoxy-2-(propylamino)tetralins has been prepared and evaluated for affinity and efficacy at dopamine (DA) D-2A receptors. The novel compounds appeared to be antagonists or inverse agonists. (R)-2-[(Benzyl)propylamino]-5-methoxytetralin (7) was characterized as a potent inverse agonists at DA D-2A receptors in a [S-35]GTP gamma S binding assay. (C) 1999 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(99)00345-5

文献信息

• Substituted 1,2,3,4-tetrahydronaphthalene derivatives
  申请人：Astra Aktiebolag

  公开号：US06124283A1

  公开（公告）日：2000-09-26

  New piperidinyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula ##STR1## wherein X is N or CH; Y is NR.sub.2 CH.sub.2, CH.sub.2 --NR.sub.2, NR.sub.2 --CO, CO--NR.sub.2 or NR.sub.2 SO.sub.2 ; R.sub.1 is H, C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.6 cycloalkyl; R.sub.3 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or (CH.sub.2).sub.n -aryl, where aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted; n is 0-4; as (R)-enantiomer, (S)-enantiomer or a racemate in the form of the free base or a pharmaceutically acceptable salt or hydrate thereof; a pharmaceutical formulation containing the compounds, use of the compounds in the treatment of 5-hydroxytryptamine mediated disorders, processes for the preparation of the compounds and intermediates for the preparation of the compounds.

  新的哌啶基或哌嗪基取代的1,2,3,4-四氢萘衍生物具有以下结构式：##STR1## 其中X为N或CH；Y为NR.sub.2 CH.sub.2，CH.sub.2--NR.sub.2，NR.sub.2--CO，CO--NR.sub.2或NR.sub.2 SO.sub.2；R.sub.1为H，C.sub.1-C.sub.6烷基或C.sub.3-C.sub.6环烷基；R.sub.3为C.sub.1-C.sub.6烷基，C.sub.3-C.sub.6环烷基或(CH.sub.2).sub.n-芳基，其中芳基为苯基或含有N、O和S中的一个或两个杂原子的杂芳环，可以是单取代或双取代；n为0-4；作为(R)-对映体，(S)-对映体或自由碱形式或其药学上可接受的盐或水合物的混合物；含有这些化合物的药物配方，这些化合物在治疗5-羟色胺介导的疾病中的用途，制备这些化合物的方法以及制备这些化合物的中间体。
• SUBSTITUTED 1,2,3,4-TETRAHYDRONAPHTHALENE DERIVATIVES
  申请人：AstraZeneca AB

  公开号：EP0888319B1

  公开（公告）日：2003-01-29
• US6124283A
  申请人：——

  公开号：US6124283A

  公开（公告）日：2000-09-26
• US6410530B1
  申请人：——

  公开号：US6410530B1

  公开（公告）日：2002-06-25
• Derivatives of (R)-2-amino-5-methoxytetralin: Antagonists and inverse agonists at the dopamine D2a receptor
  作者：Berit Backlund Höök、Cecilia Brege、Tero Linnanen、Åsa Mikaels、Åsa Malmberg、Anette M. Johansson

  DOI：10.1016/s0960-894x(99)00345-5

  日期：1999.8

  A series of N-arylmethyl substituted (R)-5-methoxy-2-(propylamino)tetralins has been prepared and evaluated for affinity and efficacy at dopamine (DA) D-2A receptors. The novel compounds appeared to be antagonists or inverse agonists. (R)-2-[(Benzyl)propylamino]-5-methoxytetralin (7) was characterized as a potent inverse agonists at DA D-2A receptors in a [S-35]GTP gamma S binding assay. (C) 1999 Elsevier Science Ltd. All rights reserved.