2-氨基-7-甲氧基四氢萘 | 4003-89-8

• 物质功能分类: 生物化工 - 提取物 - 植物提取物
• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 中文名称: 2-氨基-7-甲氧基四氢萘
• 中文别名: 7-甲氧基-1,2,3,4-四氢萘-2-胺
• 英文名称: 2-amino-7-methoxy-1,2,3,4-tetrahydronaphthalene
• 英文别名: 7-Methoxy-1,2,3,4-tetrahydronaphthalen-2-amine
• CAS: 4003-89-8
• 化学式: C₁₁H₁₅NO
• 分子量: 177.246
• InChiKey: ZNWNWWLWFCCREO-UHFFFAOYSA-N

物化性质

• 熔点：
  218-220°C
• 沸点：
  299.6±40.0 °C(Predicted)
• 密度：
  1.056±0.06 g/cm3(Predicted)
• 溶解度：
  少许溶于甲醇

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  35.2
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-氨基-7-甲氧基四氢萘 在 palladium diacetate 一氧化碳 、 1,3-双(二苯基膦)丙烷 、 氢溴酸 、 溶剂黄146 、 三乙胺 作用下， 以 二氯甲烷 、 水 、 N,N-二甲基甲酰胺 、 甲苯 为溶剂， 反应 9.33h， 生成 methyl 3-(tert-butoxycarbonylamino)tetralin-6-carboxylate
  参考文献：
  名称：

  SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF

  摘要：

  本发明提供了公式(I)的化合物： 其中R1、R1b、R2a、R2b、R2c和R2d的值如说明书中所述，可用作HDAC6的抑制剂。本发明还提供了包含本发明化合物的药物组合物，以及使用这些组合物治疗增殖性、炎症性、感染性、神经性或心血管疾病或失调的方法。

  公开号：

  US20120015943A1
• 作为产物：
  描述：

  2,7-二羟基萘 在 platinum(IV) oxide 、 palladium on activated charcoal 盐酸 、 sodium hydroxide 、 乙醇 、 氢气 、 sodium 、 对甲苯磺酸 作用下， 以 乙醇 、 苯 为溶剂， 45.0~55.0 ℃ 、303.98 kPa 条件下， 反应 26.0h， 生成 2-氨基-7-甲氧基四氢萘
  参考文献：
  名称：

  2-Amido-8-methoxytetralins: A series of nonindolic melatonin-like agents

  摘要：

  A series of unsubstituted and methoxy-substituted 2-amidotetralins (4a-q) was prepared and evaluated for their ability to compete for 2-[I-125]iodomelatonin binding to chicken retinal membranes and for their potency to inhibit the calcium-dependent release of [H-3]dopamine from rabbit retina. The lead compound, 2-acetamido-8-methoxytetralin (4j), showed a moderate affinity (K(i) = 46 nM) and potency (IC50 = 1.4 nM) at the melatonin receptor. The structural requirements necessary for optimal agonistic activity at the melatonin receptor are as follows. First, the amido group, which should have a small, nonbranched alkyl group, is essential for affinity, and second, the methoxy substituent at the 8-position of the 2-amidotetralin ring is essential for optimal agonistic activity at the melatonin receptor. We concluded that this series of unsubstituted and methoxy-substituted 2-amidotetralins constitutes a class of nonindolic melatonin-like agents that can be used as pharmacological tools to further characterize melatonin receptors and to elucidate the mode of action of melatonin.

  DOI：

  10.1021/jm00072a008

文献信息

• PREPARATION OF AMINOTETRALIN COMPOUNDS
  申请人：Gould Alexandra E.

  公开号：US20100197924A1

  公开（公告）日：2010-08-05

  The present invention relates to synthetic processes for preparation of aminotetralin compounds with kinase inhibitory activity. The invention also provides synthetic intermediates useful in the processes of the invention.

  本发明涉及用于制备具有激酶抑制活性的氨基四氢吡啶化合物的合成过程。该发明还提供了在本发明的过程中有用的合成中间体。
• Aryloxypropanolaminotetralins, a process for their preparation and
  申请人：Elf Sanofi

  公开号：US05254595A1

  公开（公告）日：1993-10-19

  Aryloxypropanolaminotetralins with beta-antagonist activity of the formula ##STR1## wherein R is hydrogen, hydroxy or methoxy and Ar is an optionally substituted aromatic or heteroaromatic group, in optically active or inactive form as well as their acid addition salts are described. A process for their preparation and pharmaceutical compositions containing the compounds of formula (i) or their pharmaceutically acceptable acid addition salts, are also described.

  具有β-阻断活性的芳氧基丙醇胺四氢萘，其通式为##STR1##，其中R为氢、羟基或甲氧基，Ar为可选择性取代的芳香或杂芳香基团，以光学活性或非活性形式及其酸加成盐被描述。它们的制备方法以及含有通式(i)化合物或其药学上可接受的酸加成盐的药物组合物也被描述。
• Conformationally defined adrenergic agents. 15. Conformationally restricted and conformationally defined tyramine analogs as inhibitors of phenylethanolamine N-methyltransferase
  作者：Qizhuang Ye、Gary L. Grunewald

  DOI：10.1021/jm00122a032

  日期：1989.2

  with m- and p-tyramine (9 and 10, respectively) is likely due to the restriction of the side-chain conformation. The conformationally defined analogues 22-24 were less active than the conformationally restricted ones, 12-15, although the low-energy half-chair conformation of 2-aminotetralin is defined in 22-24. The reduced activity of 22-24 compared with the activity of 12-15 is probably due to the

  在寻找肾上腺素合成酶苯基乙醇胺N-甲基转移酶（PNMT; EC 2.1.1.28）的选择性抑制剂，酚2-氨基四氢化萘（酪胺的构象受限类似物为12-15）和酚苯并双环[3.2.1]辛胺（使用22-24作为酪胺的构象定义类似物）来获得有关天然底物去甲肾上腺素在PNMT活性位点上的儿茶酚羟基的结合相互作用的信息。另外，这些类似物提供了有关构象柔性对酚性苯基乙胺中氨基乙基侧链的活性位相互作用的影响的信息，这可能有助于学习去甲肾上腺素在PNMT活性位点结合的方式。类似物22-24通过九步序列合成，其中，Friedel-Crafts型分子内环化是苯并双环[3.2.1]辛烷骨架构建的关键步骤。对-酪胺（10，Ki = 294 microM）比苯乙胺（1，Ki = 854 microM）更有效，但间-酪胺（9，Ki = 1250 microM）比苯基乙胺（作为PNMT抑制剂）的效力更弱。同样，在构象受限和
• Process for the preparation of substituted tetralin and substituted indane derivatives
  申请人：Zhang-Plasket Fan

  公开号：US20050240049A1

  公开（公告）日：2005-10-27

  The present invention relates to novel processes for the preparation of substituted tetralin. and substituted indane derivatives. The present invention is further directed to novel processes for the preparation of intermediates in the preparation of the substituted tetralin and substituted indane derivatives.

  本发明涉及一种制备取代四氢萘和取代茚衍生物的新工艺。本发明还涉及一种用于制备取代四氢萘和取代茚衍生物中间体的新工艺。
• Amide compounds for the potentiation of cholinergic activity
  申请人：Fujisawa Pharmaceutical Co. Ltd.

  公开号：US20030096847A1

  公开（公告）日：2003-05-22

  Amide compounds of the formula: 1 wherein R 1 and R 2 are taken together to form lower alkenylene, etc., R 3 is aryl, etc., X is N, etc., Y is a single bond, etc., and Q is 2 and salt thereof, which are useful as medicament.

  该公式的酰胺化合物：其中R1和R2一起形成较低的烯烃基，R3是芳基，X是N，Y是单键，Q是2和其盐，可用作药物。