Tert-butyl 3-(7-methoxy-3-pyrazin-2-ylpyrazolo[1,5-a]pyrimidin-5-yl)piperidine-1-carboxylate | 930595-92-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡唑并嘧啶类
• 英文名称: Tert-butyl 3-(7-methoxy-3-pyrazin-2-ylpyrazolo[1,5-a]pyrimidin-5-yl)piperidine-1-carboxylate
• CAS: 930595-92-9
• 化学式: C₂₁H₂₆N₆O₃
• 分子量: 410.476
• InChiKey: GSPZOAQIYBVSAX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  94.7
• 氢给体数：
  0
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  Tert-butyl 3-(3-iodo-7-methoxypyrazolo[1,5-a]pyrimidin-5-yl)piperidine-1-carboxylate 、 2-三丁基甲锡烷基噻唑 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 作用下， 以 1,4-二氧六环 为溶剂， 反应 12.0h， 以45%的产率得到Tert-butyl 3-(7-methoxy-3-pyrazin-2-ylpyrazolo[1,5-a]pyrimidin-5-yl)piperidine-1-carboxylate
  参考文献：
  名称：

  Methods for inhibiting protein kinases

  摘要：

  本发明提供了使用吡唑并[1,5-a]嘧啶化合物抑制选自AKT、检查点激酶、极光激酶、Pim激酶和酪氨酸激酶的蛋白激酶的方法，以及使用这些化合物治疗、预防、抑制或改善与蛋白激酶相关的一种或多种疾病的方法。

  公开号：

  US20070082900A1

文献信息

• Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors
  申请人：Guzi J. Timothy

  公开号：US20070072881A1

  公开（公告）日：2007-03-29

  In its many embodiments, the present invention provides a class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
• METHODS FOR INHIBITING PROTEIN KINASES
  申请人：Guzi Timothy J.

  公开号：US20100125068A1

  公开（公告）日：2010-05-20

  The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim kinases, and tyrosine kinase using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds.
• US7605155B2
  申请人：——

  公开号：US7605155B2

  公开（公告）日：2009-10-20
• US8211854B2
  申请人：——

  公开号：US8211854B2

  公开（公告）日：2012-07-03
• [EN] NOVEL PYRAZOLOPYRIMIDINES AS CYCLIN DEPENDENT KINASE INHIBITORS<br/>[FR] NOUVELLES PYRAZOLOPYRIMIDINES SERVANT D'INHIBITEURS DE KINASES CYCLINE-DÉPENDANTES
  申请人：SCHERING CORP

  公开号：WO2008045267A2

  公开（公告）日：2008-04-17

  [EN] In its many embodiments, the present invention provides a class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
  [FR] Dans ses différents modes de réalisation, l'invention concerne une classe de composés de pyrazolo[1,5-a]pyrimidine servant d'inhibiteurs de kinases cycline-dépendantes (CDK). L'invention concerne des procédés de préparation de tels composés, des compositions pharmaceutiques contenant au moins un de ces composés, des procédés de préparation de formulations pharmaceutiques comprenant au moins un de ces composés, et des procédés de traitement, de prévention, d'inhibition, ou d'amélioration d'au moins une maladie associée aux CDK, faisant appel à de tels composés ou à de telles compositions pharmaceutiques.