2-溴-5,6-二甲氧基-3-硝基吡啶 | 79491-48-8

• 物质功能分类: 医药中间体 - 杂环化合物 - 吡啶类化合物
• 分子结构分类: 有机化合物 - 有机1,3-偶极化合物 - 烯丙基型1,3-偶极有机化合物
• 中文名称: 2-溴-5,6-二甲氧基-3-硝基吡啶
• 英文名称: 2-bromo-5,6-dimethoxy-3-nitropyridine
• CAS: 79491-48-8
• 化学式: C₇H₇BrN₂O₄
• 分子量: 263.048
• InChiKey: FVBNYAYTCCNKSG-UHFFFAOYSA-N

物化性质

• 熔点：
  142-143 °C(Solv: methanol (67-56-1))
• 沸点：
  312.9±37.0 °C(Predicted)
• 密度：
  1.657

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  77.2
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-溴-5,6-二甲氧基-3-硝基吡啶 在 palladium 10% on activated carbon 、 氢气 作用下， 以 甲醇 为溶剂， 反应 16.0h， 以99%的产率得到5,6-dimethoxypyridin-3-amine hydrobromide
  参考文献：
  名称：

  Phosphoinositide-3-kinase inhibitors: Evaluation of substituted alcohols as replacements for the piperazine sulfonamide portion of AMG 511

  摘要：

  Replacement of the piperazine sulfonamide portion of the PI3K alpha inhibitor AMG 511 (1) with a range of aliphatic alcohols led to the identification of a truncated gem-dimethylbenzylic alcohol analog, 2-(5-(4-amino- 6-methyl-1,3,5-triazin-2-yl)-6-((5-fluoro-6-methoxypyridin-3-yl) amino) pyridin-3-yl) propan-2-ol (7). This compound possessed good in vitro efficacy and pharmacokinetic parameters and demonstrated an EC50 of 239 ng/mL in a mouse liver pharmacodynamic model measuring the inhibition of hepatocyte growth factor (HGF)-induced Akt Ser473 phosphorylation in CD1 nude mice 6 h post-oral dosing. (C) 2014 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2014.10.085
• 作为产物：
  描述：

  2,6-二溴-3-甲氧基-5-硝基吡啶 在 sodium methylate 作用下， 以 甲醇 为溶剂， 反应 20.0h， 以95%的产率得到2-溴-5,6-二甲氧基-3-硝基吡啶
  参考文献：
  名称：

  Clark, Gary J.; Deady, Leslie W., Australian Journal of Chemistry, 1981, vol. 34, # 4, p. 927 - 932

  摘要：

  DOI：

文献信息

• [EN] COMPOUNDS FOR THE TREATMENT OF KINASE-DEPENDENT DISORDERS<br/>[FR] COMPOSÉS DESTINÉS AU TRAITEMENT DE TROUBLES DÉPENDANT DE LA KINASE
  申请人：EXELIXIS INC

  公开号：WO2019148043A1

  公开（公告）日：2019-08-01

  Disclosed herein are compounds of Formula I'. Compounds of Formula I' inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase- dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

  本文披露了公式I'的化合物。公式I'的化合物抑制、调节和/或调控激酶受体，尤其是与细胞活动变化相关的Axl和Mer信号传导途径，包含这些化合物的组合物，并使用它们治疗激酶依赖性疾病和病况的方法。本发明还提供了制备上述化合物的方法和包含这些化合物的组合物。
• Thiophene-imidazopyridines
  申请人：4SC AG

  公开号：EP2017277A1

  公开（公告）日：2009-01-21

  The invention relates to thiophene-imidazopyridine compounds according to formula (I), wherein the substituents and symbols are as defined in the description. The compounds are inhibitors of PIk1.

  该发明涉及按照公式(I)的噻吩-咪唑吡啶化合物，其中取代基和符号如描述中所定义。这些化合物是PIk1的抑制剂。
• THIOPHENE-IMIDAZOPYRIDINES
  申请人：Stengel Thomas

  公开号：US20100278833A1

  公开（公告）日：2010-11-04

  The invention relates to thiophene-imidazopyridine compounds according to formula (I), wherein the substituents and symbols are as defined in the description. The compounds are inhibitors of PIk1.

  本发明涉及具有以下式（I）的噻吩-咪唑吡啶化合物，其中取代基和符号如描述中所定义。该化合物是PIk1的抑制剂。
• COMPOUNDS FOR THE TREATMENT OF KINASE-DEPENDENT DISORDERS
  申请人：Exelixis, Inc.

  公开号：EP3743068A1

  公开（公告）日：2020-12-02
• Compounds for the Treatment of Kinase-Dependent Disorders
  申请人：Exellxis, Inc.

  公开号：US20210040099A1

  公开（公告）日：2021-02-11

  Disclosed herein are compounds of Formula (I′). Compounds of Formula (I′) inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.