N-(1R,2S)-2-(2-fluoroethoxy)-2,3-DIHYDRO-1H-INDEN-1-YL-3,6-DIETHYL-5-[(4-METHYLPYRIDIN-2-YL)oxy]pyrazin-2-amine

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: N-(1R,2S)-2-(2-fluoroethoxy)-2,3-DIHYDRO-1H-INDEN-1-YL-3,6-DIETHYL-5-[(4-METHYLPYRIDIN-2-YL)oxy]pyrazin-2-amine
• 英文别名: 3,6-diethyl-N-((1R,2S)-2-(2-fluoroethoxy)-2,3-dihydro-1H-inden-1-yl)-5-(4-methylpyridin-2-yloxy)pyrazin-2-amine；3,6-diethyl-N-[(1R,2S)-2-(2-fluoroethoxy)-2,3-dihydro-1H-inden-1-yl]-5-(4-methylpyridin-2-yl)oxypyrazin-2-amine
• 化学式: C₂₅H₂₉FN₄O₂
• 分子量: 436.529
• InChiKey: CZDYVVMDBOUYST-JTHBVZDNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.1
• 重原子数：
  32
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  69.2
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  (1R,2S)-1-({3,6-diethyl-5-[(4-methylpyridin-2-yl)oxy]pyrazin-2-yl}amino)-2,3-dihydro-1H-inden-2-ol 、 alkaline earth salt of/the/ methylsulfuric acid 在 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 N-(1R,2S)-2-(2-fluoroethoxy)-2,3-DIHYDRO-1H-INDEN-1-YL-3,6-DIETHYL-5-[(4-METHYLPYRIDIN-2-YL)oxy]pyrazin-2-amine
  参考文献：
  名称：

  Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists

  摘要：

  Low nanomolar corticotropin releasing factor type-1 (CRF1) receptor antagonists containing unique indanylamines were identified from the heteroatom-linked pyrazine chemotype. The most potent indanylpyrazine had a K-i = 11 +/- 1 nM. The oxygen-linked pyrazinyl derivatives were prepared through a copper-catalyzed coupling of a pyridinone to a bromo- or iodopyrazine. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.09.008

文献信息

• Substituted 1,4-pyrazine derivatives
  申请人：——

  公开号：US20040116444A1

  公开（公告）日：2004-06-17

  Substituted aryl 1,4-pyrazine derivatives and their use in treating anxiety disorders, depression and stress related disorders are disclosed.

  本发明揭示了取代芳基1,4-吡嗪衍生物及其在治疗焦虑症、抑郁症和与压力相关的疾病中的应用。
• Heteroatom-linked indanylpyrazines are corticotropin releasing factor type-1 receptor antagonists
  作者：Jeffrey W. Corbett、Mark R. Rauckhorst、Fang Qian、Robert L. Hoffman、Christopher S. Knauer、Lawrence W. Fitzgerald

  DOI：10.1016/j.bmcl.2007.09.008

  日期：2007.11

  Low nanomolar corticotropin releasing factor type-1 (CRF1) receptor antagonists containing unique indanylamines were identified from the heteroatom-linked pyrazine chemotype. The most potent indanylpyrazine had a K-i = 11 +/- 1 nM. The oxygen-linked pyrazinyl derivatives were prepared through a copper-catalyzed coupling of a pyridinone to a bromo- or iodopyrazine. (C) 2007 Elsevier Ltd. All rights reserved.