3-(6-(2-(4-Fluorophenyl)pyrrolidin-1-yl)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amine | 1169687-45-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 3-(6-(2-(4-Fluorophenyl)pyrrolidin-1-yl)pyrimidin-4-yl)pyrazolo[1,5-a]pyrimidin-2-amine
• 英文别名: 3-[6-[2-(4-fluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]pyrazolo[1,5-a]pyrimidin-2-amine
• CAS: 1169687-45-9
• 化学式: C₂₀H₁₈FN₇
• 分子量: 375.408
• InChiKey: WNDJXHTVTVODGW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  28
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  85.2
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  2-(4-氟苯基)吡咯烷 、 3-(6-(methylsulfinyl)pyrimidin-4-yl)-pyrazolo[1,5-a]pyrimidin-2-amine 以 N-甲基吡咯烷酮 为溶剂， 生成 3-(6-(2-(4-Fluorophenyl)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

文献信息

• PYRAZOLO[1,5-a]PYRIMIDINES USEFUL AS JAK2 INHIBITORS
  申请人：LEDEBOER Mark

  公开号：US20110118255A1

  公开（公告）日：2011-05-19

  The present invention relates to compounds of formula (I) useful as selective inhibitors of JAK2 kinase. The invention also provides pharmaceutical acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various diseases, conditions or disorders. The invention also provides processes for preparing the compounds of the invention.

  本发明涉及公式(I)的化合物，其作为JAK2激酶的选择性抑制剂有用。本发明还提供了包含该化合物的药学可接受组合物以及使用该组合物治疗各种疾病、病症或障碍的方法。本发明还提供了制备该发明化合物的过程。
• US8937064B2
  申请人：——

  公开号：US8937064B2

  公开（公告）日：2015-01-20
• 2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2
  作者：Mark W. Ledeboer、Albert C. Pierce、John P. Duffy、Huai Gao、David Messersmith、Francesco G. Salituro、Suganthini Nanthakumar、Jon Come、Harmon J. Zuccola、Lora Swenson、Dina Shlyakter、Sudipta Mahajan、Thomas Hoock、Bin Fan、Wan-Jung Tsai、Elaine Kolaczkowski、Scott Carrier、James K. Hogan、Richard Zessis、S. Pazhanisamy、Youssef L. Bennani

  DOI：10.1016/j.bmcl.2009.10.053

  日期：2009.12

  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.