6-甲氧基-1,2,3,4-四氢萘-2-胺 | 70312-05-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 中文名称: 6-甲氧基-1,2,3,4-四氢萘-2-胺
• 英文名称: 2-amino-6-methoxy-1,2,3,4-tetrahydronaphthalene
• 英文别名: (-)-2-amino-1,2,3,4-tetrahydro-6-methoxynaphthalene；6-methoxy-1,2,3,4-tetrahydronaphthalen-2-ylamine；6-methoxytetralin-2-amine；2-amino-6-methoxytetralin；6-methoxy-1,2,3,4-tetrahydro-naphthalen-2-ylamine；2-Amino-6-methoxy-1,2,3,4-tetrahydronaphtalene；6-methoxy-1,2,3,4-tetrahydronaphthalen-2-amine
• CAS: 70312-05-9；70312-07-1；81861-30-5
• 化学式: C₁₁H₁₅NO
• mdl: MFCD04114915
• 分子量: 177.246
• InChiKey: WASIYUSITZITPW-UHFFFAOYSA-N

物化性质

• 沸点：
  299.6±40.0 °C(Predicted)
• 密度：
  1.056±0.06 g/cm3(Predicted)

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：
  0.454
• 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：

  6-甲氧基-1,2,3,4-四氢萘-2-胺 在 三溴化硼 作用下， 以 二氯甲烷 为溶剂， 生成 6-氨基-5,6,7,8-四氢萘-2-醇
  参考文献：
  名称：

  DE2803582

  摘要：

  公开号：
• 作为产物：
  描述：

  2,6-萘二酚 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 6-甲氧基-1,2,3,4-四氢萘-2-胺
  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

• DPP IV inhibitors
  申请人：——

  公开号：US20030130281A1

  公开（公告）日：2003-07-10

  The present invention relates to compounds of formula (I) 1 wherein R 1 , R 2 , and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.

  本发明涉及以下式（I）的化合物： 其中R1、R2和X如描述和权利要求中所定义，并且其药学上可接受的盐。这些化合物可用于治疗和/或预防与DPP IV相关的疾病，如糖尿病，特别是非胰岛素依赖型糖尿病和糖耐量受损。
• Synthesis of phenethylamine moiety by photoamination of styrene derivatives with ammonia
  作者：Toshiaki Yamashita、Masabide Yasuda、Toshihiro Isami、Shozo Nakano、Kimiko Tanabe、Kensuke Shima

  DOI：10.1016/s0040-4039(00)60695-0

  日期：1993.8

  The photoaminations of trans-1-arylpropenes and 7-methoxy-1,2-dihydronaphthalenes with ammonia in the presence of dicyanobenzene gave 1-aryl-2-propylamines and 2-amino-6-methoxy-1,2,3,4-tetrahydronaphthalenes, respectively. The yields of the aminated compounds were improved by the addition of 1,3,5-triphenylbenzene or m-terphenyl.

  在二氰基苯存在下，反式-1-芳基丙烯和7-甲氧基-1,2-二氢萘与氨光胺化，得到1-芳基-2-丙胺和2-氨基-6-甲氧基-1,2,3,4-四氢萘分别。通过添加1,3,5-三苯苯或间三联苯可提高胺化化合物的收率。
• [EN] AUTOTAXIN INHIBITORS<br/>[FR] INHIBITEURS DE L'AUTOTAXINE
  申请人：MERCK PATENT GMBH

  公开号：WO2010112124A1

  公开（公告）日：2010-10-07

  The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.

  本发明涉及按照式(I)的化合物作为自体脂肪酶抑制剂，以及利用这种化合物治疗和/或预防由增加的溶酶磷脂酸水平和/或自体脂肪酶的激活引起、介导和/或传播的生理和/或病理条件，特别是不同癌症的治疗。
• [EN] PYRIMIDINE AMIDE COMPOUNDS<br/>[FR] COMPOSÉS PYRIMIDINE AMIDE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2012123467A1

  公开（公告）日：2012-09-20

  Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.

  本文提供的化合物为式(I)的化合物及其药学上可接受的盐，其中取代基如规范中所披露的那样。这些化合物及含有它们的药物组合物对于治疗炎症性疾病和紊乱，例如哮喘和慢性阻塞性肺病（COPD）等，具有实用性。
• [EN] SUBSTITUTED TETRALINS AND INDANES AND THEIR USE<br/>[FR] TETRALINES ET INDANES SUBSTITUES ET LEUR UTILISATION
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2004037779A1

  公开（公告）日：2004-05-06

  This invention features tetralin and indane compounds, compositions containing them, and methods of using them as PPAR alpha modulators to treat or inhibit the progression of, for example, diabetes.

  这项发明涉及四氢萘和茚烷化合物，含有它们的组合物，以及将它们用作PPARα调节剂来治疗或抑制例如糖尿病等疾病进展的方法。