1-[6-(1H-indazol-4-yl)-8-morpholin-4-ylimidazo[1,2-a]pyrazin-3-yl]piperidin-4-amine | 1252595-28-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡唑类
• 英文名称: 1-[6-(1H-indazol-4-yl)-8-morpholin-4-ylimidazo[1,2-a]pyrazin-3-yl]piperidin-4-amine
• CAS: 1252595-28-0
• 化学式: C₂₂H₂₆N₈O
• 分子量: 418.501
• InChiKey: IOSYKFVVXIKDRU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  31
• 可旋转键数：
  3
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  101
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  2-氨基-5-溴-3-吗啉-4-基吡嗪 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 potassium carbonate 作用下， 以 乙二醇二甲醚 、 1,2-二氯乙烷 为溶剂， 反应 0.5h， 生成 1-[6-(1H-indazol-4-yl)-8-morpholin-4-ylimidazo[1,2-a]pyrazin-3-yl]piperidin-4-amine
  参考文献：
  名称：

  New use of bis(benzotriazolyl)-1,2-(dialkylamino)ethanes for the synthesis of 2-H-3-dialkylamino imidazo[1,2-a]pyrazine derivatives

  摘要：

  First direct synthesis of 2-H-3-N-dialkyl-imidazo[1,2-a]pyrazines is described. This approach makes use of accessible substituted pyrazines and the assistance of benzotriazole. In such a manner we accomplished the introduction of cyclic amines at C-3 of the scaffold in a convenient formal cyclisation procedure. Detailed examples and utility of this approach are presented herein. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2011.12.077

文献信息

• IMIDAZOPYRAZINES AS INHIBITORS OF PROTEIN KINASES
  申请人：Centro Nacional de Investigaciones Oncológicas (CNIO)

  公开号：EP2419429B1

  公开（公告）日：2014-03-26
• New use of bis(benzotriazolyl)-1,2-(dialkylamino)ethanes for the synthesis of 2-H-3-dialkylamino imidazo[1,2-a]pyrazine derivatives
  作者：Joaquín Pastor、Sonsoles Rodríguez-Arístegui、Ana Isabel Hernández、Carmen Varela、Antonio Salgado、Sonia Martínez

  DOI：10.1016/j.tetlet.2011.12.077

  日期：2012.2

  First direct synthesis of 2-H-3-N-dialkyl-imidazo[1,2-a]pyrazines is described. This approach makes use of accessible substituted pyrazines and the assistance of benzotriazole. In such a manner we accomplished the introduction of cyclic amines at C-3 of the scaffold in a convenient formal cyclisation procedure. Detailed examples and utility of this approach are presented herein. (C) 2011 Elsevier Ltd. All rights reserved.