5-[(3-aminophenyl)ethynyl]pyrimidin-2-amine | 857264-92-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 5-[(3-aminophenyl)ethynyl]pyrimidin-2-amine
• 英文别名: 5-[2-(3-aminophenyl)ethynyl]pyrimidin-2-amine
• CAS: 857264-92-7
• 化学式: C₁₂H₁₀N₄
• 分子量: 210.238
• InChiKey: BAMHGZKSROSDGC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  77.8
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  5-[(3-aminophenyl)ethynyl]pyrimidin-2-amine 、 氯甲酸苯酯 在 吡啶 作用下， 以 四氢呋喃 为溶剂， 反应 2.0h， 以94%的产率得到phenyl (3-[(2-aminopyrimidin-5-yl)ethynyl]phenyl)carbamate
  参考文献：
  名称：

  WO2006/82373

  摘要：

  公开号：
• 作为产物：
  描述：

  3-氨基苯乙炔 在 bis-triphenylphosphine-palladium(II) chloride 、 copper(l) iodide 三乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 2.0h， 以60%的产率得到5-[(3-aminophenyl)ethynyl]pyrimidin-2-amine
  参考文献：
  名称：

  WO2006/82373

  摘要：

  公开号：

文献信息

• Aminopyrimidine Derivatives With Tie2 Inhibiting Activity
  申请人：Jones Clifford David

  公开号：US20080194552A1

  公开（公告）日：2008-08-14

  The invention relates to a compound of the Formula I or salt thereof wherein R x , R y , R x , R 5 , R 6 , A, B, L, n and m are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm blooded animal. The invention also relates to processes for the preparation of said compounds.

  该发明涉及式I化合物或其盐，其中Rx、Ry、Rx、R5、R6、A、B、L、n和m如描述中所定义。该发明还涉及所述化合物的药物组合物，所述化合物作为药物的用途以及在温血动物中产生抗血管生成作用的生产。该发明还涉及所述化合物的制备方法。
• [EN] PYRIMIDINES WITH TIE2 (TEK) ACTIVITY<br/>[FR] PYRIMIDINES A ACTIVITE TIE2 (TEK)
  申请人：ASTRAZENECA AB

  公开号：WO2005060970A1

  公开（公告）日：2005-07-07

  The invention relates to a compound of the Formula (I). or salt thereof wherein R1, R2, R3, R4, R5, R6, A, B, L, n and m are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm-blooded animal. The invention also relates to processes for the preparation of said compounds.

  该发明涉及公式(I)的化合物或其盐，其中R1、R2、R3、R4、R5、R6、A、B、L、n和m如描述中所定义。该发明还涉及所述化合物的药物组合物，所述化合物作为药物以及在温血动物中产生抗血管生成效应的用途。该发明还涉及所述化合物的制备方法。
• Pyrimidines With Tie2 (Tek) Activity
  申请人：Jones Clifford David

  公开号：US20080108608A1

  公开（公告）日：2008-05-08

  The invention relates to a compound of the Formula (I). or salt thereof wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , A, B, L, n and m are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm-blooded animal. The invention also relates to processes for the preparation of said compounds.

  该发明涉及一种式（I）的化合物或其盐，其中R1、R2、R3、R4、R5、R6、A、B、L、n和m在描述中定义。该发明还涉及所述化合物的制药组合物，所述化合物作为药物和在温血动物中产生抗血管生成效应的用途以及制备所述化合物的方法。
• Pyrimidine Compounds Having Tie-2 (Tek) Inhibitory Activity
  申请人：Jones Clifford David

  公开号：US20080146599A1

  公开（公告）日：2008-06-19

  The invention relates to a compound of the Formula (I) or salt, prodrug or solvate thereof, wherein R x , R y , R z , R 5 , R 6 , A, B, L, n and m are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm blooded animal. The invention also relates to processes for the preparation of said compounds.

  本发明涉及公式（I）的化合物或其盐、前药或溶剂化物，其中Rx、Ry、Rz、R5、R6、A、B、L、n和m的定义如说明书所述。本发明还涉及所述化合物的药物组合物，所述化合物作为药物的使用以及在温血动物中产生抗血管生成效应的生产。本发明还涉及制备所述化合物的方法。
• PYRIMIDINE COMPOUNDS HAVING TIES (TEK) INHIBITORY ACTIVITY
  申请人：Jones Clifford David

  公开号：US20100048543A1

  公开（公告）日：2010-02-25

  The invention relates to a compound of the Formula I or salt thereof wherein R x , R y , R z , R 5 , R 6 , A, B, L, n and m are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm-blooded animal. The invention also relates to processes for the preparation of said compounds.

  本发明涉及公式I的化合物或其盐，其中Rx，Ry，Rz，R5，R6，A，B，L，n和m如描述中所定义。本发明还涉及该化合物的药物组合物，该化合物作为药物使用以及在恒温动物中产生抗血管生成效应的生产。本发明还涉及制备该化合物的过程。