4-(3-氯-2-氟苯胺)-6,7-二羟基喹唑啉 | 848440-15-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 4-(3-氯-2-氟苯胺)-6,7-二羟基喹唑啉
• 英文名称: 4-(3-chloro-2-fluoroanilino)-6,7-dihydroxyquinazoline
• 英文别名: 4-(3-chloro-2-fluoro-anilino)quinazoline-6,7-diol；4-(3-chloro-2-fluoroanilino)quinazoline-6,7-diol
• CAS: 848440-15-3
• 化学式: C₁₄H₉ClFN₃O₂
• 分子量: 305.696
• InChiKey: MAHMVNIYVAYDOD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  78.3
• 氢给体数：
  3
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  4-(3-氯-2-氟苯胺)-6,7-二羟基喹唑啉 在 polystyrene-supported triphenylphosphine 、 氨 、 三乙胺 作用下， 以 四氢呋喃 、 甲醇 、 二氯甲烷 为溶剂， 反应 7.0h， 生成
  参考文献：
  名称：

  Selective alkylation of a 6,7-dihydroxyquinazoline

  摘要：

  A convenient 3-step multi-parallel process for the preparation of 4-(3-chloro-2-fluoroanilino)-6,7-bisalkoxyquinazolines is highlighted. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2005.09.038
• 作为产物：
  描述：

  6,7-二甲氧基喹唑啉-4-酮 在 吡啶 、 甲烷磺酸 、 吡啶盐酸盐 、 DL-蛋氨酸 作用下， 以 异丙醇 为溶剂， 反应 25.0h， 生成 4-(3-氯-2-氟苯胺)-6,7-二羟基喹唑啉
  参考文献：
  名称：

  Selective alkylation of a 6,7-dihydroxyquinazoline

  摘要：

  A convenient 3-step multi-parallel process for the preparation of 4-(3-chloro-2-fluoroanilino)-6,7-bisalkoxyquinazolines is highlighted. (c) 2005 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetlet.2005.09.038

文献信息

• [EN] COMPOSITIONS AND METHODS FOR TREATING CANCER<br/>[FR] COMPOSITIONS ET MÉTHODES DE TRAITEMENT DU CANCER
  申请人：UNIV CALIFORNIA

  公开号：WO2019067543A1

  公开（公告）日：2019-04-04

  The present disclosure relates to compounds that are capable penetrating to the blood brain barrier to modulate the activity of EGFR tyrosine kinase. The disclosure further relates to methods of treating Glioblastoma and other EGFR mediated cancers. The disclosure further relates to methods of treating Glioblastoma and other EGFR mediated cancers that have been determined to have altered glucose metabolism in the presence of inhibitors. The present dislcsoure also provides methods oadministering to a subject a glucose metabolism inhibitor and a cytoplasmic p53 stabilizer.

  本公开涉及能够穿透血脑屏障以调节EGFR酪氨酸激酶活性的化合物。该公开进一步涉及治疗胶质母细胞瘤和其他EGFR介导的癌症的方法。该公开还涉及治疗已确定在抑制剂存在下具有改变葡萄糖代谢的胶质母细胞瘤和其他EGFR介导的癌症的方法。本公开还提供了向受试者施用葡萄糖代谢抑制剂和细胞质p53稳定剂的方法。
• [EN] QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS<br/>[FR] DERIVES DE QUINAZOLINE UTILISES COMME INHIBITEURS DE LA TYROSINE KINASE
  申请人：ASTRAZENECA AB

  公开号：WO2005026150A1

  公开（公告）日：2005-03-24

  The invention concerns quinazoline derivatives of the Formula (I); wherein each of R1, R2, W, X1, X2, Z, a and b are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula (I) are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, particularly EGFR tyrosine kinase.

  该发明涉及配方（I）的喹唑啉衍生物；其中R1、R2、W、X1、X2、Z、a和b在描述中有定义；它们的制备方法；含有它们的药物组合物以及它们在制造用于提供抗增殖效果的药物的用途。配方（I）的喹唑啉衍生物预计在治疗某些由erbB受体酪氨酸激酶介导的癌症等疾病中具有用处，特别是EGFR酪氨酸激酶。
• [EN] NOVEL FLUORINATED DERIVATIVES AS EGFR INHIBITORS USEFUL FOR TREATING CANCERS<br/>[FR] NOUVEAUX DÉRIVÉS FLUORÉS UTILISÉS EN TANT QU'INHIBITEURS D'EGFR UTILES POUR LE TRAITEMENT DE CANCERS
  申请人：TRILLIUM THERAPEUTICS INC

  公开号：WO2016123706A1

  公开（公告）日：2016-08-11

  A novel class of fluorinated derivatives of Formula I have been prepared and found to be useful in the treatment of cancers and other EGFR related disorders.

  一类新型的Formula I的氟化衍生物已经被制备出来，并发现在治疗癌症和其他与EGFR相关的疾病方面非常有用。
• Quinazoline derivatives as tyrosine kinase inhibitors
  申请人：Hennequin Andre Laurent Francois

  公开号：US20070043009A1

  公开（公告）日：2007-02-22

  The invention concerns quinazoline derivatives of the Formula (I); wherein each of R 1 , R 2 , W, X 1 , X 2 , Z, a and b are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula (I) are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, particularly EGFR tyrosine kinase.

  该发明涉及式（I）的喹唑啉衍生物；其中R1，R2，W，X1，X2，Z，a和b的定义如描述中所述；它们的制备过程；含有它们的药物组合物及其用于制造提供抗增殖效应的药物的用途。预计式（I）的喹唑啉衍生物可用于治疗由erbB受体酪氨酸激酶介导的某些癌症等疾病，特别是EGFR酪氨酸激酶。
• QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITORS
  申请人：HENNEQUIN Laurent Francois Andre

  公开号：US20090312343A1

  公开（公告）日：2009-12-17

  The invention concerns quinazoline derivatives of the Formula I: wherein each of R 1 , R 2 , W, X 1 , X 2 , Z, a and b are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula I are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, particularly EGFR tyrosine kinase.

  本发明涉及式I的喹唑啉衍生物：其中R1、R2、W、X1、X2、Z、a和b如描述中所定义;它们的制备方法; 包含它们的制药组合物，以及它们在制造提供抗增殖效应的药物方面的用途。式I的喹唑啉衍生物预计可用于治疗某些由erbB受体酪氨酸激酶介导的癌症，特别是EGFR酪氨酸激酶。