3-(2-chloro-5-methoxypyrimidin-4-yl)imidazo[1,2-a]pyridine | 1224708-14-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: 3-(2-chloro-5-methoxypyrimidin-4-yl)imidazo[1,2-a]pyridine
• CAS: 1224708-14-8
• 化学式: C₁₂H₉ClN₄O
• 分子量: 260.683
• InChiKey: WRDRQXUJWODFET-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  52.3
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  2-氨基吡啶 、 (E)-2-chloro-4-(2-ethoxyvinyl)-5-methoxypyrimidine 在 N-溴代丁二酰亚胺(NBS) 作用下， 以 1,4-二氧六环 、 水 为溶剂， 反应 3.0h， 以42%的产率得到3-(2-chloro-5-methoxypyrimidin-4-yl)imidazo[1,2-a]pyridine
  参考文献：
  名称：

  NOVEL COMPOUNDS 515

  摘要：

  提供了化学式（I）的新型嘧啶衍生物或其药用盐，以及它们的制备方法、含有它们的药物组合物以及它们在治疗中的应用。

  公开号：

  US20100105655A1

文献信息

• Derivatives of N-cycloalkyl/heterocycloalkyl-4-(imidazo[1,2-a]pyridine)pyrimidin-2-amine as therapeutic agents
  申请人：Aucentra Therapeutics Pty Ltd

  公开号：US11111245B2

  公开（公告）日：2021-09-07

  A novel class of inhibitors of protein kinases that are useful in the treatment of cell proliferative diseases and conditions, and especially those characterised by over-expression of one or more CDK enzyme and/or by one or more aberrant CDK activity, including certain cancers of lung, breast, brain, ovary, prostate, colorectal cancer and leukaemias. The inhibitors have the general structure (I).

  一类新型蛋白激酶抑制剂，可用于治疗细胞增殖性疾病和病症，特别是以一种或多种 CDK 酶过度表达和/或一种或多种 CDK 活性异常为特征的疾病和病症，包括某些肺癌、乳腺癌、脑癌、卵巢癌、前列腺癌、结直肠癌和白血病。这些抑制剂具有一般结构 (I)。
• A versatile route to 3-(pyrimidin-4-yl)-imidazo[1,2-a]pyridines and 3-(pyrimidin-4-yl)-pyrazolo[1,5-a]pyridines
  作者：Richard Ducray、Pascal Boutron、Myriam Didelot、Hervé Germain、Franck Lach、Maryannick Lamorlette、Antoine Legriffon、Mickael Maudet、Morgan Ménard、Georges Pasquet、Fabrice Renaud、Iain Simpson、Gail L. Young

  DOI：10.1016/j.tetlet.2010.07.024

  日期：2010.9

  A two-step synthesis of 3-(2-chloropyrimidin-4-yl)imidazo[1,2-a]pyridines is presented. The late stage elaboration of the imidazopyridine through a cyclocondensation allows a rapid access to a variety of substitution patterns. The intermediate enol ethers were obtained from inexpensive reagents in a ligand-free Heck coupling. This methodology has been extended to the formation of pyrazolo[1,5-a]pyridines via a formal 1,3-dipolar cycloaddition. (C) 2010 Elsevier Ltd. All rights reserved.
• DERIVATIVES OF N-CYCLOALKYL/HETEROCYCLOALKYL-4-(IMIDAZO[1,2-a]PYRIDINE)PYRIMIDIN-2-AMINE AS THERAPEUTIC AGENTS
  申请人：Aucentra Therapeutics Pty Ltd

  公开号：US20200231586A1

  公开（公告）日：2020-07-23

  A novel class of inhibitors of protein kinases that are useful in the treatment of cell proliferative diseases and conditions, and especially those characterised by over-expression of one or more CDK enzyme and/or by one or more aberrant CDK activity, including certain cancers of lung, breast, brain, ovary, prostate, colorectal cancer and leukaemias. The inhibitors have the general structure (I).
• [EN] PYRAZOLO- AND IMIDAZOPYRIDINYLPYRIMIDINEAMINES AS IGF-1R TYROSINE KINASE INHIBITORS<br/>[FR] PYRAZOLO ET IMIDAZO-PYRIDINYL-PYRIMIDINAMINES UTILISÉS COMME INHIBITEURS DE LA TYROSINE KINASE IGF-1R
  申请人：ASTRAZENECA AB

  公开号：WO2010049731A1

  公开（公告）日：2010-05-06

  There is provided novel pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
• NOVEL COMPOUNDS 515
  申请人：Ducray Richard

  公开号：US20100105655A1

  公开（公告）日：2010-04-29

  There is provided novel pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

  提供了化学式（I）的新型嘧啶衍生物或其药用盐，以及它们的制备方法、含有它们的药物组合物以及它们在治疗中的应用。