4-chloro-8-fluoroimidazo[1,2-a] quinoxaline

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 4-chloro-8-fluoroimidazo[1,2-a] quinoxaline
• 英文别名: 4-Chloro-8-fluoroimidazo[1,2-a]quinoxaline
• 化学式: C₁₀H₅ClFN₃
• 分子量: 221.621
• InChiKey: DGXWCFWUCFNNLI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  15
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  30.2
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-chloro-8-fluoroimidazo[1,2-a] quinoxaline 、 环己胺 以 乙醇 为溶剂， 生成 4-cyclohexylamino-8-fluoroimidazo[1,2-a]quinoxalin
  参考文献：
  名称：

  Imidazo[1,2-a]quinoxalin-4-amines: A novel class of nonxanthine A1-adenosine receptor antagonists

  摘要：

  The syntheses and A(1) adenosine receptor affinities of a number of imidazo[1,2-alpha]quinoxalin-4-amines are reported. Structure activity relationships within the series and in comparison with other similar tricyclic nonxanthine adenosine antagonists are discussed, leading to a putative common binding mode of these nitrogen-containing heterocycles to A(1) adenosine receptors. Secondary amino compounds displayed the best affinities toward A(1) receptors, while the tertiary amines were almost devoid of activity, thus suggesting a crucial role for the hydrogen bond-forming 4-NH group. Remarkably higher potencies for l-methyl and N-cyclopentyl derivatives were also found. 4-Cyclopentylamino-1-methylimidazo[1,2-alpha]quinoxaline (IRFI 165) is the most potent compound in this series, having K-i(A(1)) = 7.9 nM. It is also provided with a good A(1) selectivity both versus A(2a) and A(3) subtypes and was selected for further pharmacological studies. (C) Elsevier, Paris.

  DOI：

  10.1016/s0223-5234(99)80019-1
• 作为产物：
  描述：

  4-氟-1,2-苯二胺 在 氢溴酸 、 N,N-二甲基苯胺 、 三氯氧磷 作用下， 以 乙醇 为溶剂， 反应 40.0h， 生成 4-chloro-8-fluoroimidazo[1,2-a] quinoxaline
  参考文献：
  名称：

  Imidazo[1,2-a]quinoxalin-4-amines: A novel class of nonxanthine A1-adenosine receptor antagonists

  摘要：

  The syntheses and A(1) adenosine receptor affinities of a number of imidazo[1,2-alpha]quinoxalin-4-amines are reported. Structure activity relationships within the series and in comparison with other similar tricyclic nonxanthine adenosine antagonists are discussed, leading to a putative common binding mode of these nitrogen-containing heterocycles to A(1) adenosine receptors. Secondary amino compounds displayed the best affinities toward A(1) receptors, while the tertiary amines were almost devoid of activity, thus suggesting a crucial role for the hydrogen bond-forming 4-NH group. Remarkably higher potencies for l-methyl and N-cyclopentyl derivatives were also found. 4-Cyclopentylamino-1-methylimidazo[1,2-alpha]quinoxaline (IRFI 165) is the most potent compound in this series, having K-i(A(1)) = 7.9 nM. It is also provided with a good A(1) selectivity both versus A(2a) and A(3) subtypes and was selected for further pharmacological studies. (C) Elsevier, Paris.

  DOI：

  10.1016/s0223-5234(99)80019-1

文献信息

• [EN] SUBSTITUTED IMIDAZOQUINOXALINES<br/>[FR] IMIDAZOQUINOXALINES SUBSTITUÉES
  申请人：BAYER SCHERING PHARMA AG

  公开号：WO2010124826A1

  公开（公告）日：2010-11-04

  The present invention relates to substituted imidazoquinoxaline compounds of general formula (I) as inhibitors of Mps-1 Kinase or TTK, and being active against inflammation and cancer.

  本发明涉及一种通式（I）的替代咪唑喹喔啉化合物，作为Mps-1激酶或TTK的抑制剂，并对炎症和癌症具有活性。
• SUBSTITUTED IMIDAZOQUINOXALINES
  申请人：Koppitz Marcus

  公开号：US20120128662A1

  公开（公告）日：2012-05-24

  The present invention relates to substituted imidazoquinoxaline compounds of general formula (I) as inhibitors of Mps-1 Kinase or TTK, and being active against inflammation and cancer.

  本发明涉及通式（I）的取代咪唑喹噁啉化合物，作为Mps-1激酶或TTK的抑制剂，并对炎症和癌症具有活性。
• US6124287
  申请人：——

  公开号：——

  公开（公告）日：——
• US06124287
  申请人：——

  公开号：——

  公开（公告）日：——
• IMIDAZO 1,2-a]QUINOXALIN-4-AMINES ACTIVE AS ADENOSINE ANTAGONISTS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS THEREOF
  申请人：Biomedica Foscama Industria Chimico-Farmaceutica S.p.A.

  公开号：EP0865442A1

  公开（公告）日：1998-09-23