N-cyclopentyl-4-[5,7-dichloro-2-(4-fluorophenyl)pyrazolo(1,5-a]pyridin-3-yl]-2-pyrimidinamine | 474303-67-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: N-cyclopentyl-4-[5,7-dichloro-2-(4-fluorophenyl)pyrazolo(1,5-a]pyridin-3-yl]-2-pyrimidinamine
• 英文别名: N-cyclopentyl-4-[5,7-dichloro-2-(4-fluorophenyl)pyrazolo[1,5-a]pyridin-3-yl]pyrimidin-2-amine
• CAS: 474303-67-8
• 化学式: C₂₂H₁₈Cl₂FN₅
• 分子量: 442.323
• InChiKey: ZKYXVDDZBFULBP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.9
• 重原子数：
  30
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  55.1
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  N-cyclopentyl-4-[5,7-dichloro-2-(4-fluorophenyl)pyrazolo(1,5-a]pyridin-3-yl]-2-pyrimidinamine 、 环戊胺 在 palladium diacetate caesium carbonate 、 R-(+)-1,1'-联萘-2,2'-双二苯膦 作用下， 反应 24.0h， 以68%的产率得到N-{4-[5-chloro-7-(cyclopentylamino)-2-(4-fluorophenyl)pyrazolo[1,5-a]pyridin-3-yl]-2-pyrimidinyl}-N-cyclopentylamine
  参考文献：
  名称：

  Pyrazolopyridines with potent activity against herpesviruses: Effects of C5 substituents on antiviral activity

  摘要：

  Synthesis of a series of 5-substituted as well as 5,7-disubstituted 3-[2-(cyclopentylamino)-4-pyrimidinyl]-2-phenylpyrazolo [1,5-a]pyridin-7-amines with potent activity against herpes simplex viruses is described. Synthetic approaches allowing for variation of the substitution pattern are outlined and resulting changes in antiviral activity are highlighted. Several compounds with in vitro antiviral activity similar to or better than acyclovir are described. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.11.120
• 作为产物：
  描述：

  4-[5-chloro-2-(4-fluorophenyl)pyrazolo[1,5-a]pyridin-3-yl]-N-cyclopentyl-2-pyrimidinamine 在 正丁基锂 、 四氯化碳 作用下， 以 四氢呋喃 为溶剂， 以45%的产率得到N-cyclopentyl-4-[5,7-dichloro-2-(4-fluorophenyl)pyrazolo(1,5-a]pyridin-3-yl]-2-pyrimidinamine
  参考文献：
  名称：

  Pyrazolopyridines with potent activity against herpesviruses: Effects of C5 substituents on antiviral activity

  摘要：

  Synthesis of a series of 5-substituted as well as 5,7-disubstituted 3-[2-(cyclopentylamino)-4-pyrimidinyl]-2-phenylpyrazolo [1,5-a]pyridin-7-amines with potent activity against herpes simplex viruses is described. Synthetic approaches allowing for variation of the substitution pattern are outlined and resulting changes in antiviral activity are highlighted. Several compounds with in vitro antiviral activity similar to or better than acyclovir are described. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2007.11.120

文献信息

• Pyrazolopyridinyl pyridine and pyrimidine therapeutic compounds
  申请人：Gudmundsson Kristjan

  公开号：US20050192295A1

  公开（公告）日：2005-09-01

  The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.

  本发明提供了公式（I）的化合物：其中所有变量如本文所定义，包含该化合物的制药组合物，制备该化合物的过程以及它们作为制药剂的用途。
• Therapeutic compounds
  申请人：——

  公开号：US20040142941A1

  公开（公告）日：2004-07-22

  The present invention provides compounds of formula (I), pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents. 1

  本发明提供了式（I）化合物，包含其的制药组合物，制备该化合物的过程以及其用作制药剂的用途。
• PYRAZOLO[1,5-A]PYRIDINE DERIVATIVES
  申请人：SmithKline Beecham Corporation

  公开号：EP1385847B1

  公开（公告）日：2005-06-01
• US6962914B2
  申请人：——

  公开号：US6962914B2

  公开（公告）日：2005-11-08
• US7030134B2
  申请人：——

  公开号：US7030134B2

  公开（公告）日：2006-04-18