4-chloro-6-morpholinoquinoline | 878276-84-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 4-chloro-6-morpholinoquinoline
• 英文别名: 4-(4-Chloroquinolin-6-yl)morpholine
• CAS: 878276-84-7
• 化学式: C₁₃H₁₃ClN₂O
• 分子量: 248.712
• InChiKey: HICMHZRUSMTWJV-UHFFFAOYSA-N

物化性质

• 沸点：
  408.0±45.0 °C(Predicted)
• 密度：
  1.295±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.31
• 拓扑面积：
  25.4
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-chloro-6-morpholinoquinoline 在 tris-(dibenzylideneacetone)dipalladium(0) 、 甲酸 、 caesium carbonate 、 4,5-双二苯基膦-9,9-二甲基氧杂蒽 作用下， 以 1,4-二氧六环 、 N,N-二甲基甲酰胺 为溶剂， 反应 14.0h， 生成 N-(6-(5-((2-methylpyridin-4-yl)amino)-1H-benzo[d]imidazol-2-yl)pyridin-3-yl)-6-morpholinoquinolin-4-amine
  参考文献：
  名称：

  [EN] AKT3 MODULATORS
  [FR] MODULATEURS DE AKT3

  摘要：

  公式Ia、Ib或Ic的化合物已被描述，其中各种取代基在此定义。这些化合物可以在体外或体内调节Akt3的性质或效果，并且也可以单独或与其他药剂结合在预防或治疗各种疾病方面使用。描述了合成这些化合物的方法。还描述了制药组合物以及使用这些化合物或组合物在预防或治疗各种疾病中单独或与其他药剂或组合物结合的方法。

  公开号：

  WO2021226519A1
• 作为产物：
  描述：

  6-morpholin-4-yl-quinolin-4-ol 在 三氯氧磷 作用下， 反应 3.0h， 生成 4-chloro-6-morpholinoquinoline
  参考文献：
  名称：

  Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities

  摘要：

  A simple two-step synthesis method was used to make 51 B-ring-substituted 4-hydroxyquinolines allowing analysis of the effect of ring substitutions on inhibition of growth of chloroquine sensitive and resistant strains of Plasmodium falciparum, the dominant cause of malaria morbidity. Substituted quinoline rings other than the 7-chloroquinoline ring found in chloroquine were found to have significant activity against the drug-resistant strain of P. falciparum W2. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.12.037

文献信息

• [EN] AKT3 MODULATORS<br/>[FR] MODULATEURS DE AKT3
  申请人：GEORGIAMUNE LLC

  公开号：WO2021226519A1

  公开（公告）日：2021-11-11

  Compounds of Formula la, lb, or Ic, are described, where the various substituents are defined herein. The compounds can modulate a property or effect of Akt3 in vitro or in vivo, and can also be used, individually or in combination with other agents, in the prevention or treatment of a variety of conditions. Methods for synthesizing the compounds are described. Pharmaceutical compositions and methods of using these compounds or compositions, individually or in combination with other agents or compositions, in the prevention or treatment of a variety of conditions are also described.

  公式Ia、Ib或Ic的化合物已被描述，其中各种取代基在此定义。这些化合物可以在体外或体内调节Akt3的性质或效果，并且也可以单独或与其他药剂结合在预防或治疗各种疾病方面使用。描述了合成这些化合物的方法。还描述了制药组合物以及使用这些化合物或组合物在预防或治疗各种疾病中单独或与其他药剂或组合物结合的方法。
• Successive substitution of halogen atoms in 4, 6-dihaloquinolines in palladium-catalyzed reactions with amines and arylboronic acids
  作者：I. P. Beletskaya、A. V. Tsvetkov、P. V. Tsvetkov、G. V. Latyshev、N. V. Lukashev

  DOI：10.1007/s11172-005-0239-y

  日期：2005.1

  A procedure was developed for the synthesis of 4,6-diamino- and 4,6- or 6,4-arylaminoquinolines by palladium-catalyzed C-N- and/or C-C-cross-coupling of 6-bromo-4-chloroquinoline.

  开发了一种通过钯催化的 6-溴-4-氯喹啉的 CN-和/或 CC-交叉偶联合成 4,6-二氨基和 4,6- 或 6,4-芳基氨基喹啉的程序。
• [EN] AKT3 MODULATORS<br/>[FR] MODULATEURS D'AKT3
  申请人：GEORGIAMUNE LLC

  公开号：WO2021226517A1

  公开（公告）日：2021-11-11

  Compounds of Formula la, lb, or Ic,, are described, where the various substituents are defined herein. The compounds can modulate a property or effect of Akt3 in vitro or in vivo, and can also be used, individually or in combination with other agents, in the prevention or treatment of a variety of conditions. Methods for synthesizing the compounds are described. Pharmaceutical compositions and methods of using these compounds or compositions, individually or in combination with other agents or compositions, in the prevention or treatment of a variety of conditions are also described.

  公式Ia、Ib或Ic的化合物被描述，其中各种取代基在此处被定义。这些化合物可以在体外或体内调节Akt3的性质或效应，并且也可以单独或与其他药剂结合在预防或治疗各种疾病方面使用。描述了合成这些化合物的方法。还描述了使用这些化合物或组合物的药物组合物和使用这些化合物或组合物，单独或与其他药剂或组合物结合在预防或治疗各种疾病方面的方法。
• Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities
  作者：Peter B. Madrid、John Sherrill、Ally P. Liou、Jennifer L. Weisman、Joseph L. DeRisi、R. Kiplin Guy

  DOI：10.1016/j.bmcl.2004.12.037

  日期：2005.2

  A simple two-step synthesis method was used to make 51 B-ring-substituted 4-hydroxyquinolines allowing analysis of the effect of ring substitutions on inhibition of growth of chloroquine sensitive and resistant strains of Plasmodium falciparum, the dominant cause of malaria morbidity. Substituted quinoline rings other than the 7-chloroquinoline ring found in chloroquine were found to have significant activity against the drug-resistant strain of P. falciparum W2. (C) 2004 Elsevier Ltd. All rights reserved.