2-(2-chloro-4-nitrophenoxy)pyridine | 871020-94-9

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-(2-chloro-4-nitrophenoxy)pyridine
• CAS: 871020-94-9
• 化学式: C₁₁H₇ClN₂O₃
• 分子量: 250.641
• InChiKey: KIMYWZDNYDXOSN-UHFFFAOYSA-N

物化性质

• 沸点：
  344.7±32.0 °C(Predicted)
• 密度：
  1.415±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  17
• 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：
  67.9
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-(2-chloro-4-nitrophenoxy)pyridine 在 platinum on activated charcoal 、 氢气 作用下， 以 乙醇 为溶剂， 生成 3-chloro-4-(pyridin-2-yloxy)aniline
  参考文献：
  名称：

  Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors

  摘要：

  Aniline 'headgroups' were synthesized and incorporated into an alkynyl thienopyrimidine series of EGFR and ErbB-2 inhibitors. Potent inhibition of enzyme activity and cellular proliferation was observed. In certain instances, protein binding was reduced and oral exposure was found to be somewhat improved relative to compounds containing the reference aniline. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.01.080
• 作为产物：
  描述：

  2-羟基吡啶 、 3-氯-4-氟硝基苯 在 sodium hydride 作用下， 反应 18.5h， 以43%的产率得到2-(2-chloro-4-nitrophenoxy)pyridine
  参考文献：
  名称：

  [EN] QUINAZOLINE DERIVATIVES AS ERBB RECEPTOR TYROSINE KINASES
  [FR] DERIVES DE QUINAZOLINE UTILISES COMME TYROSINE KINASES DU RECEPTEUR ERBB

  摘要：

  该发明涉及公式(I)的喹唑啉衍生物，其中R1、R2、R3、R4、R5、R6、R7、X1、Q1、m和n中的每个都具有描述中定义的任意含义；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作抗增殖剂的药物中的用途，用于预防或治疗对erbB受体酪氨酸激酶抑制敏感的肿瘤。

  公开号：

  WO2005118572A1

文献信息

• Quinazoline Derivatives as Erbb Receptor Tyrosine kinases
  申请人：Bradbury Hugh Robert

  公开号：US20070232607A1

  公开（公告）日：2007-10-04

  The invention concerns quinazoline derivatives of the formula (I), wherein each of R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X 1 , Q 1 , m and n have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.

  这项发明涉及公式（I）的喹唑啉衍生物，其中R1、R2、R3、R4、R5、R6、R7、X1、Q1、m和n中的每一个都具有描述中定义的任何含义；它们的制备过程，含有它们的制药组合物以及它们在制造用作抗增殖剂的药物的过程中的使用，用于预防或治疗对erbB受体酪氨酸激酶抑制敏感的肿瘤。
• QUINAZOLINE DERIVATIVES AS ERBB RECEPTOR TYROSINE KINASES
  申请人：AstraZeneca AB

  公开号：EP1756088A1

  公开（公告）日：2007-02-28
• Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors
  作者：Alex G. Waterson、Kimberly G. Petrov、Keith R. Hornberger、Robert D. Hubbard、Douglas M. Sammond、Stephon C. Smith、Hamilton D. Dickson、Thomas R. Caferro、Kevin W. Hinkle、Kirk L. Stevens、Scott H. Dickerson、David W. Rusnak、Glenn M. Spehar、Edgar R. Wood、Robert J. Griffin、David E. Uehling

  DOI：10.1016/j.bmcl.2009.01.080

  日期：2009.3

  Aniline 'headgroups' were synthesized and incorporated into an alkynyl thienopyrimidine series of EGFR and ErbB-2 inhibitors. Potent inhibition of enzyme activity and cellular proliferation was observed. In certain instances, protein binding was reduced and oral exposure was found to be somewhat improved relative to compounds containing the reference aniline. (C) 2009 Elsevier Ltd. All rights reserved.
• [EN] QUINAZOLINE DERIVATIVES AS ERBB RECEPTOR TYROSINE KINASES<br/>[FR] DERIVES DE QUINAZOLINE UTILISES COMME TYROSINE KINASES DU RECEPTEUR ERBB
  申请人：ASTRAZENECA AB

  公开号：WO2005118572A1

  公开（公告）日：2005-12-15

  The invention concerns quinazoline derivatives of the formula (I), wherein each of R1, R2, R3, R4, R5, R6, R7, X1, Q1, m and n have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.

  该发明涉及公式(I)的喹唑啉衍生物，其中R1、R2、R3、R4、R5、R6、R7、X1、Q1、m和n中的每个都具有描述中定义的任意含义；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作抗增殖剂的药物中的用途，用于预防或治疗对erbB受体酪氨酸激酶抑制敏感的肿瘤。