3-(6-(3-(Dimethylamino)pyrrolidin-1-yl)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amine | 1202225-68-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 3-(6-(3-(Dimethylamino)pyrrolidin-1-yl)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amine
• 英文别名: 3-[6-[3-(dimethylamino)pyrrolidin-1-yl]pyrimidin-4-yl]pyrazolo[1,5-a]pyrimidin-2-amine
• CAS: 1202225-68-0
• 化学式: C₁₆H₂₀N₈
• 分子量: 324.388
• InChiKey: JODJTZLGTGMBHR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  24
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  88.5
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  3-(6-(methylsulfinyl)pyrimidin-4-yl)-pyrazolo[1,5-a]pyrimidin-2-amine 、 3-(二甲氨基)吡咯烷 以 N-甲基吡咯烷酮 为溶剂， 生成 3-(6-(3-(Dimethylamino)pyrrolidin-1-yl)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amine
  参考文献：
  名称：

  2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2

  摘要：

  Constitutive activation of the EPO/JAK2 signaling cascade has recently been implicated in a variety of myeloproliferative disorders including polycythemia vera, essential thrombocythemia and myelofibrosis. In an effort to uncover therapeutic potential of blocking the EPO/JAK2 signaling cascade, we sought to discover selective inhibitors that block the kinase activity of JAK2. Herein, we describe the discovery and structure based optimization of a novel series of 2-amino-pyrazolo[1,5-a]pyrimidines that exhibit potent inhibition of JAK2. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.10.053