2-(quinazolin-2-yl)phenol | 25171-16-8

• 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: 2-(quinazolin-2-yl)phenol
• 英文别名: 2--chinazolin；2-Quinazolin-2-ylphenol
• CAS: 25171-16-8
• 化学式: C₁₄H₁₀N₂O
• 分子量: 222.246
• InChiKey: PBYCJOHNHBEVLT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  17
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  46
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  水杨醛 、 2-氨基苄胺 在 3-硝基吡啶 作用下， 以 乙腈 为溶剂， 反应 16.0h， 以94%的产率得到2-(quinazolin-2-yl)phenol
  参考文献：
  名称：

  在有氧条件下利用有机催化多米诺战略发散合成喹唑啉

  摘要：

  基于有机催化的多米诺反应，描述了一种方便的合成2-取代的喹唑啉的方法。在开发的条件下，探索了各种各样的底物，并以高收率获得了所需的产品。

  DOI：

  10.1002/ejoc.201800746

文献信息

• [EN] THERAPEUTIC OXY-PHENYL-ARYL COMPOUNDS AND THEIR USE<br/>[FR] COMPOSÉS OXY-PHÉNYL-ARYLES THÉRAPEUTIQUES ET LEUR UTILISATION
  申请人：CANCER REC TECH LTD

  公开号：WO2009053694A1

  公开（公告）日：2009-04-30

  The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain oxy phenyl aryl compounds (referred to herein as OPA compounds), as described herein, which, inter alia, inhibit Checkpoint Kinase 2 (CHK2) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK2 kinase function, and in the treatment of diseases and conditions that are mediated by CHK2, that are ameliorated by the inhibition of CHK2 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.

  本发明总体涉及治疗化合物领域，更具体地涉及如本文所述的某些氧基苯基芳基化合物（以下简称OPA化合物），其中，抑制检查点激酶2（CHK2）激酶功能。本发明还涉及包含此类化合物的药物组合物，以及使用此类化合物和组合物，在体内外抑制CHK2激酶功能，以及治疗由CHK2介导的疾病和状况，包括通过抑制CHK2激酶功能而改善的疾病和状况，等等，包括诸如癌症等增殖性疾病，可选地与另一剂联合使用，例如，（a）DNA拓扑异构酶I或II抑制剂；（b）DNA损伤剂；（c）抗代谢物或TS抑制剂；（d）针对微管的药剂；（e）电离辐射。
• Niacin as a Potent Organocatalyst towards the Synthesis of Quinazolines Using Nitriles as C-N Source
  作者：Raghuram Gujjarappa、Nagaraju Vodnala、Velma Ganga Reddy、Chandi C. Malakar

  DOI：10.1002/ejoc.201901651

  日期：2020.2.21

  An organocatalyzed protocol has been described for the comprehensive synthesis of 2‐substituted quinazolines using nitriles as C–N source. The developed reaction conditions are suitable for a wide range of substrates providing the desired products in excellent yields.

  已经描述了使用腈作为CN来源全面合成2取代的喹唑啉的有机催化方案。所开发的反应条件适用于各种底物，以优异的产率提供所需的产物。
• ULTRAVIOLET LIGHT ABSORBERS
  申请人：Transitions Optical, Inc.

  公开号：US20170275534A1

  公开（公告）日：2017-09-28

  The present invention relates to compounds that have ultraviolet light absorbing properties, and which can also have mesogenic properties. The present invention also relates to compositions that include one or more such compounds, and to articles of manufacture that include one or more such compounds, such as optical elements that include an optical substrate and a layer that includes at least one compound of the present invention.

  本发明涉及具有吸收紫外光特性的化合物，该化合物还可以具有介向性质。本发明还涉及包括一种或多种这种化合物的组合物，以及包括一种或多种这种化合物的制造物，例如包括光学基底和包含本发明至少一种化合物的层的光学元件。
• Therapeutic Oxy-Phenyl-Aryl Compounds and Their Use
  申请人：Collins Ian

  公开号：US20110201592A1

  公开（公告）日：2011-08-18

  The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain oxy phenyl aryl compounds (referred to herein as OPA compounds), as described herein, which, inter alia, inhibit Checkpoint Kinase 2 (CHK2) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK2 kinase function, and in the treatment of diseases and conditions that are mediated by CHK2, that are ameliorated by the inhibition of CHK2 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.

  本发明涉及治疗化合物领域，更具体地涉及某些氧苯基芳基化合物（以下简称OPA化合物），如本文所述，该化合物在其中抑制检查点激酶2（CHK2）激酶功能。本发明还涉及包含这种化合物的制药组合物，以及在体外和体内使用这种化合物和组合物来抑制CHK2激酶功能，并治疗由CHK2介导，通过抑制CHK2激酶功能改善的疾病和病况，包括增殖性疾病，如癌症等，可选择与另一种药物一起使用，例如（a）DNA拓扑异构酶I或II抑制剂；（b）DNA损伤剂；（c）抗代谢物或TS抑制剂；（d）微管靶向药物；和（e）电离辐射。
• Copper-catalyzed synthesis of quinazolines <i>via</i> cascade cyclization/hydrodehalogenation
  作者：Peng Ma、Yuhang Wang、Jianhui Wang、Ning Ma

  DOI：10.1039/d3nj00541k

  日期：——

  We report a Cu(I)-catalyzed synthesis of quinazolines via cascade cyclization/hydrodehalogenation by using acetamide as a nitrogen source and H2O as a hydrogen source. The current reaction provides a unified modular route from readily available starting materials to quinazolines in which aryl aldehydes can be decorated with diverse substitutions. In this reaction, acetamide becomes an interesting alternative

  我们报道了使用乙酰胺作为氮源和 H 2 O 作为氢源，通过级联环化/加氢脱卤，Cu( I ) 催化合成喹唑啉。目前的反应提供了一个统一的模块化路线，从容易获得的起始材料到喹唑啉，其中芳基醛可以用不同的取代物进行修饰。在这个反应中，乙酰胺成为令人不快的氨和有毒脒的有趣替代品。