N-[4-(2-甲氧基苯氧基)苯基]-3-吡啶甲胺 | 353235-63-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: N-[4-(2-甲氧基苯氧基)苯基]-3-吡啶甲胺
• 中文别名: 4-(2-甲氧基苯氧基)-N-(吡啶-3-甲基)苯胺
• 英文名称: N-[4-(2-methoxyphenoxy)phenyl]pyridin-3-ylmethylamine
• 英文别名: 4-(2-methoxyphenoxy)-N-(pyridin-3-ylmethyl)aniline
• CAS: 353235-63-9
• 化学式: C₁₉H₁₈N₂O₂
• 分子量: 306.364
• InChiKey: XGIMENIGAKFWHM-UHFFFAOYSA-N

物化性质

• 密度：
  1.190

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  23
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  43.4
• 氢给体数：
  1
• 氢受体数：
  4

安全信息

• 海关编码：
  2933399090

反应信息

• 作为反应物：
  描述：

  2,2,2-三氟乙基磺酰氯 、 N-[4-(2-甲氧基苯氧基)苯基]-3-吡啶甲胺 在 吡啶 作用下， 以 1,2-二氯乙烷 为溶剂， 生成 2,2,2-三氟-N-[4-(2-甲氧基苯氧基)苯基]-N-(3-吡啶基甲基)-乙磺酰胺
  参考文献：
  名称：

  Potentiators of glutamate receptors

  摘要：

  本发明涉及代谢型谷氨酸受体功能的增强剂，具体提供了化合物I的公式、其组合物以及使用方法。

  公开号：

  US20040006114A1
• 作为产物：
  描述：

  3-吡啶甲醛 在 potassium carbonate 、 copper(II) oxide 作用下， 以 吡啶 、 甲醇 为溶剂， 反应 60.5h， 生成 N-[4-(2-甲氧基苯氧基)苯基]-3-吡啶甲胺
  参考文献：
  名称：

  Discovery of Allosteric Potentiators for the Metabotropic Glutamate 2 Receptor:  Synthesis and Subtype Selectivity of N-(4-(2-Methoxyphenoxy)phenyl)-N-(2,2,2− trifluoroethylsulfonyl)pyrid-3-ylmethylamine

  摘要：

  This report describes recently discovered novel allosteric modulators of metabotropic glutamate2 (mGlu2) receptors. These pyridylmethylsulfonamides (e.g., 3) potentiate glutamate, shifting agonist potency by 2-fold. This effect was specific for mGlu2 (vs mGlu1,3-8 receptors). Also, 3 failed to potentiate a chimeric mGlu2/1 receptor, demonstrating the mGlu2 transmembrane region's critical involvement. In a fear-potentiated startle model, 3 showed anxiolytic activity that was prevented by mGlu2/3 antagonist pretreatment. Thus, these pyridylmethylsulfonamides represent the first mGlu2 receptor potentiators discovered.

  DOI：

  10.1021/jm034015u

文献信息

• PYRIDINE DERIVATIVES AS POTENTIATORS OF GLUTAMATE RECEPTORS
  申请人：ELI LILLY AND COMPANY

  公开号：EP1255735A2

  公开（公告）日：2002-11-13
• US6800651B2
  申请人：——

  公开号：US6800651B2

  公开（公告）日：2004-10-05
• [EN] POTENTIATORS OF GLUTAMATE RECEPTORS<br/>[FR] AGENTS DE POTENTIALISATION DE RECEPTEURS DE GLUTAMATE
  申请人：LILLY CO ELI

  公开号：WO2001056990A2

  公开（公告）日：2001-08-09

  The present invention relates to potentiators of metabotropic glutamate receptor function and specifically provides compounds of formula I, compositions thereof and methods of using the same for the treatment of eg. anxiety, migraine, schizophrenia or epilepsy.
• Potentiators of glutamate receptors
  申请人：——

  公开号：US20040006114A1

  公开（公告）日：2004-01-08

  The present invention relates to potentiators of metabotropic glutamate receptor function and specifically provides compounds of formula I, compositions thereof and methods of using the same. 1

  本发明涉及代谢型谷氨酸受体功能的增强剂，具体提供了化合物I的公式、其组合物以及使用方法。
• Discovery of Allosteric Potentiators for the Metabotropic Glutamate 2 Receptor:  Synthesis and Subtype Selectivity of <i>N</i>-(4-(2-Methoxyphenoxy)phenyl)-<i>N</i>-(2,2,2− trifluoroethylsulfonyl)pyrid-3-ylmethylamine
  作者：Michael P. Johnson、Melvyn Baez、G. Erik Jagdmann、Thomas C. Britton、Thomas H. Large、David O. Callagaro、Joseph P. Tizzano、James A. Monn、Darryle D. Schoepp

  DOI：10.1021/jm034015u

  日期：2003.7.1

  This report describes recently discovered novel allosteric modulators of metabotropic glutamate2 (mGlu2) receptors. These pyridylmethylsulfonamides (e.g., 3) potentiate glutamate, shifting agonist potency by 2-fold. This effect was specific for mGlu2 (vs mGlu1,3-8 receptors). Also, 3 failed to potentiate a chimeric mGlu2/1 receptor, demonstrating the mGlu2 transmembrane region's critical involvement. In a fear-potentiated startle model, 3 showed anxiolytic activity that was prevented by mGlu2/3 antagonist pretreatment. Thus, these pyridylmethylsulfonamides represent the first mGlu2 receptor potentiators discovered.