4-(2-Butoxyethenyl)-2-chloro-5-cyclopropylpyrimidine

• 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: 4-(2-Butoxyethenyl)-2-chloro-5-cyclopropylpyrimidine
• 英文别名: 4-(2-butoxyethenyl)-2-chloro-5-cyclopropylpyrimidine
• 化学式: C₁₃H₁₇ClN₂O
• 分子量: 252.744
• InChiKey: GOAOJLIMNHRHBM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  17
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  35
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-(2-Butoxyethenyl)-2-chloro-5-cyclopropylpyrimidine 、 1-aminopyridinium iodide 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 8.0h， 以52%的产率得到3-(2-chloro-5-cyclopropyl-pyrimidin-4-yl)pyrazolo[1,5-a]pyridine
  参考文献：
  名称：

  A versatile route to 3-(pyrimidin-4-yl)-imidazo[1,2-a]pyridines and 3-(pyrimidin-4-yl)-pyrazolo[1,5-a]pyridines

  摘要：

  A two-step synthesis of 3-(2-chloropyrimidin-4-yl)imidazo[1,2-a]pyridines is presented. The late stage elaboration of the imidazopyridine through a cyclocondensation allows a rapid access to a variety of substitution patterns. The intermediate enol ethers were obtained from inexpensive reagents in a ligand-free Heck coupling. This methodology has been extended to the formation of pyrazolo[1,5-a]pyridines via a formal 1,3-dipolar cycloaddition. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2010.07.024
• 作为产物：
  描述：

  乙烯基正丁醚 、 2,4-dichloro-5-cyclopropylpyrimidine 在 palladium diacetate 、 三乙胺 作用下， 以 polyethyleneglycol-400 为溶剂， 反应 2.0h， 以47%的产率得到4-(2-Butoxyethenyl)-2-chloro-5-cyclopropylpyrimidine
  参考文献：
  名称：

  A versatile route to 3-(pyrimidin-4-yl)-imidazo[1,2-a]pyridines and 3-(pyrimidin-4-yl)-pyrazolo[1,5-a]pyridines

  摘要：

  A two-step synthesis of 3-(2-chloropyrimidin-4-yl)imidazo[1,2-a]pyridines is presented. The late stage elaboration of the imidazopyridine through a cyclocondensation allows a rapid access to a variety of substitution patterns. The intermediate enol ethers were obtained from inexpensive reagents in a ligand-free Heck coupling. This methodology has been extended to the formation of pyrazolo[1,5-a]pyridines via a formal 1,3-dipolar cycloaddition. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2010.07.024

文献信息

• NOVEL COMPOUNDS 515
  申请人：Ducray Richard

  公开号：US20100105655A1

  公开（公告）日：2010-04-29

  There is provided novel pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

  提供了化学式（I）的新型嘧啶衍生物或其药用盐，以及它们的制备方法、含有它们的药物组合物以及它们在治疗中的应用。
• [EN] PYRAZOLO- AND IMIDAZOPYRIDINYLPYRIMIDINEAMINES AS IGF-1R TYROSINE KINASE INHIBITORS<br/>[FR] PYRAZOLO ET IMIDAZO-PYRIDINYL-PYRIMIDINAMINES UTILISÉS COMME INHIBITEURS DE LA TYROSINE KINASE IGF-1R
  申请人：ASTRAZENECA AB

  公开号：WO2010049731A1

  公开（公告）日：2010-05-06

  There is provided novel pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.