thieno[2,3-b]pyridin-2-ylmethanamine | 933751-19-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩并吡啶类
• 英文名称: thieno[2,3-b]pyridin-2-ylmethanamine
• CAS: 933751-19-0
• 化学式: C₈H₈N₂S
• 分子量: 164.231
• InChiKey: BBIQTAHQJBHQDS-UHFFFAOYSA-N

物化性质

• 沸点：
  318.8±27.0 °C(Predicted)
• 密度：
  1.300±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  67.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  thieno[2,3-b]pyridin-2-ylmethanamine 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 caesium carbonate 、 溶剂黄146 、 N,N-二异丙基乙胺 、 sodium nitrite 作用下， 以 1,4-二氧六环 、 水 为溶剂， 反应 1.5h， 生成 2-((6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)methyl)thieno[2,3-b]pyridine
  参考文献：
  名称：

  Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (Volitinib) as a Highly Potent and Selective Mesenchymal–Epithelial Transition Factor (c-Met) Inhibitor in Clinical Development for Treatment of Cancer

  摘要：

  HGF/c-Met signaling has been implicated in human cancers. Herein we describe the invention of a series of novel triazolopyrazine c-Met inhibitors. The structure activity relationship of these compounds was investigated, leading to the identification of compound 28, which demonstrated favorable pharmacokinetic properties in mice and good antitumor activities in the human glioma xenograft model in athymic nude mice.

  DOI：

  10.1021/jm500510f
• 作为产物：
  描述：

  噻吩并[2,3-B!吡啶-2-甲醛 在 sodium tetrahydroborate 、 氯化亚砜 、 氨 作用下， 以 甲醇 、 二氯甲烷 为溶剂， 反应 16.58h， 生成 thieno[2,3-b]pyridin-2-ylmethanamine
  参考文献：
  名称：

  Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (Volitinib) as a Highly Potent and Selective Mesenchymal–Epithelial Transition Factor (c-Met) Inhibitor in Clinical Development for Treatment of Cancer

  摘要：

  HGF/c-Met signaling has been implicated in human cancers. Herein we describe the invention of a series of novel triazolopyrazine c-Met inhibitors. The structure activity relationship of these compounds was investigated, leading to the identification of compound 28, which demonstrated favorable pharmacokinetic properties in mice and good antitumor activities in the human glioma xenograft model in athymic nude mice.

  DOI：

  10.1021/jm500510f

文献信息

• [EN] CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR<br/>[FR] CERTAINES TRIAZOLOPYRIDINES ET TRIAZOLOPYRAZINES, LEURS COMPOSITIONS ET LEURS PROCEDES D'UTILISATION
  申请人：HUTCHISON MEDIPHARMA LTD

  公开号：WO2011079804A1

  公开（公告）日：2011-07-07

  Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.

  提供了某些三唑吡啶和三唑吡嗪，以及它们的组成物和使用方法。
• CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
  申请人：SU Wei-Guo

  公开号：US20120245178A1

  公开（公告）日：2012-09-27

  Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.

  提供了某些三唑吡啶和三唑吡嗪，以及它们的组成物和使用方法。
• CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
  申请人：Su Wei-Guo

  公开号：US20120264739A1

  公开（公告）日：2012-10-18

  Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.

  提供了某些三唑并吡啶和三唑并嘧啶，以及它们的组成物和使用方法。
• Certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor
  申请人：Su Wei-Guo

  公开号：US08507487B2

  公开（公告）日：2013-08-13

  Provided are certain triazolopyridines and triazolopyrazines of Formula 1. wherein X, Y, R1, R2, R3, R4 and R5 have any of the meanings described herein; processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of cell proliferative disorders.

  提供了一些公式1中的三唑并吡啶和三唑并嘧啶，其中X、Y、R1、R2、R3、R4和R5具有以下任何含义；它们的制备过程，包含它们的药物组合物以及它们在治疗细胞增殖性疾病中的用途。
• CERTAIN TRIAZOLOPYRIDINES, COMPOSITIONS THEREOF AND THEIR USE IN THE TREATMENT OF CANCER.
  申请人：Hutchison Medipharma Limited

  公开号：EP2966075A1

  公开（公告）日：2016-01-13

  Provided are certain triazolopyridines, compositions thereof and their use in the treatment of cancer.

  本文提供了某些三唑并吡啶、其组合物及其在治疗癌症中的用途。