N-(pyridin-2-yl)quinazolin-4-amine | 1245798-51-9

• 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: N-(pyridin-2-yl)quinazolin-4-amine
• 英文别名: N-pyridin-2-ylquinazolin-4-amine
• CAS: 1245798-51-9
• 化学式: C₁₃H₁₀N₄
• 分子量: 222.249
• InChiKey: NWUSZGRNRYCQJE-UHFFFAOYSA-N

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：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  50.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  N-(3-bromopyridin-2-yl)quinazolin-4-amine 在 10% palladium on carbon 、 氢气 、 sodium carbonate 作用下， 以 乙醇 为溶剂， 反应 3.0h， 以50%的产率得到N-(pyridin-2-yl)quinazolin-4-amine
  参考文献：
  名称：

  Synthesis of new tetracyclic azaheteroaromatic cores via auto-tandem Pd-catalyzed and one-pot Pd- and Cu-catalyzed double C–N bond formation

  摘要：

  Inter- and intramolecular transition metal-catalyzed amination of 2-chloro-3-iodopyridine and 2,3-dibromopyridine, respectively, with benzodiazinamines yielded six hitherto unknown tetracyclic azaheteroaromatic cores. C-N bond formation was achieved via auto-tandem (Pd-catalyst) as well as one-pot (sequential use of a Pd- and Cu-catalyst) catalysis. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tet.2010.06.038

文献信息

• [EN] QUINAZOLINE DERIVATIVES<br/>[FR] DÉRIVÉS QUINAZOLINIQUES
  申请人：ASTRAZENECA AB

  公开号：WO2004081000A1

  公开（公告）日：2004-09-23

  The invention concerns quinazoline derivatives of Formula (I) wherein Z is an O, S, SO, SO2, N(R2) or C(R2)(R3) group wherein each R2 or R3 group is hydrogen or (1-8C)alkyl, m is 1, 2 or 3, each R1 group is selected from halogeno, (1-8C)alkyl, (1-6C)alkoxy and any of the other meanings defined in the description, Ra is hydrogen or halogeno, Rb is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy, Rc is hydrogen, halogeno, (1-8C)alkyl or (1-6C)alkoxy, and Rd is (1-6C)alkoxy, or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.

  该发明涉及式（I）的喹唑啉衍生物，其中Z是O、S、SO、SO2、N（R2）或C（R2）（R3）基团，其中每个R2或R3基团是氢或（1-8C）烷基，m为1、2或3，每个R1基团选自卤代、（1-8C）烷基、（1-6C）烷氧基和描述中定义的其他含义，Ra为氢或卤代，Rb为氢、卤代、（1-6C）烷基或（1-6C）烷氧基，Rc为氢、卤代、（1-8C）烷基或（1-6C）烷氧基，Rd为（1-6C）烷氧基，或其药学上可接受的盐；其制备方法，含有它们的药物组合物以及它们在制造用作抗侵袭剂的药物的药物中的使用，用于固体肿瘤疾病的遏制和/或治疗。
• Synthesis of new tetracyclic azaheteroaromatic cores via auto-tandem Pd-catalyzed and one-pot Pd- and Cu-catalyzed double C–N bond formation
  作者：Tom R.M. Rauws、Claudio Biancalani、Joris W. De Schutter、Bert U.W. Maes

  DOI：10.1016/j.tet.2010.06.038

  日期：2010.8

  Inter- and intramolecular transition metal-catalyzed amination of 2-chloro-3-iodopyridine and 2,3-dibromopyridine, respectively, with benzodiazinamines yielded six hitherto unknown tetracyclic azaheteroaromatic cores. C-N bond formation was achieved via auto-tandem (Pd-catalyst) as well as one-pot (sequential use of a Pd- and Cu-catalyst) catalysis. (C) 2010 Elsevier Ltd. All rights reserved.