1-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)oxy)propan-2-one | 649736-37-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)oxy)propan-2-one
• 英文别名: 1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-one；1-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methyl-pyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-propan-2-one；1-[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxypropan-2-one
• CAS: 649736-37-8
• 化学式: C₁₉H₁₇FN₄O₃
• 分子量: 368.367
• InChiKey: YYEPDBKFCHASFG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  27
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  81.5
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  4-(4-氟-2-甲基-1H-吲哚-5-氧基)-ALPHA,ALPHA,5-三甲基吡咯并[2,1-F][1,2,4]三嗪-6-甲醇 、 一氯丙酮 、 potassium carbonate 在 ethyl acetate dichloromethane 作用下， 以 丙酮 为溶剂， 反应 6.0h， 以to afford the desired product (3.34 g, 91% yield) as a light beige solid的产率得到1-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)oxy)propan-2-one
  参考文献：
  名称：

  Novel inhibitors of kinases

  摘要：

  本发明提供了I式化合物及其药学上可接受的盐。式I化合物能够抑制生长因子受体如VEGFR-2和FGFR-1的酪氨酸激酶活性，因此可用作抗癌剂。式I化合物还可用于治疗与通过生长因子受体进行信号转导途径相关的其他疾病。

  公开号：

  US20040072832A1

文献信息

• STEREOSELECTIVE REDUCTION PROCESS FOR THE PREPARATION OF PYRROLOTRIAZINE COMPOUNDS
  申请人：Patel N. Ramesh

  公开号：US20060286646A1

  公开（公告）日：2006-12-21

  The invention relates to a process for the enzymatic, stereoselective reduction of ketone compounds to provide chiral alcohols, for example the compound of formula Ib:

  本发明涉及一种酶催化的立体选择性还原酮化合物的过程，用于提供手性醇，例如公式Ib的化合物。
• Novel inhibitors of kinases
  申请人：——

  公开号：US20040072832A1

  公开（公告）日：2004-04-15

  The present invention provides compounds of formula I, 1 and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.

  本发明提供公式I的化合物及其药学上可接受的盐。公式I的化合物抑制生长因子受体的酪氨酸激酶活性，例如VEGFR-2和FGFR-1，因此使它们成为抗癌剂。公式I的化合物还可用于治疗与信号转导途径相关的其他疾病，这些途径通过生长因子受体运作。
• NOVEL INHIBITORS OF KINASES
  申请人：Bhide S. Rajeev

  公开号：US20070299075A1

  公开（公告）日：2007-12-27

  The present invention provides compounds of formula I, and pharmaceutically acceptable salts thereof The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.

  本发明提供了I式化合物及其药学上可接受的盐。I式化合物抑制生长因子受体如VEGFR-2和FGFR-1的酪氨酸激酶活性，因此可用作抗癌剂。I式化合物还可用于治疗通过生长因子受体操作的信号转导途径引起的其他疾病。
• Stereoselective reduction process for the preparation of pyrrolotriazine compounds
  申请人：Bristol-Myers Squibb Company

  公开号：US07393667B2

  公开（公告）日：2008-07-01

  The invention relates to a process for the enzymatic, stereoselective reduction of ketone compounds to provide chiral alcohols, for example the compound of formula Ib:

  该发明涉及一种酶催化的立体选择性还原酮化合物的过程，以提供手性醇，例如化合物Ib的公式：
• Pyrrolo[2,1-f][1,2,4]triazine derivatives as kinase inhibitors
  申请人：Bristol-Myers Squibb Company

  公开号：EP2280012A2

  公开（公告）日：2011-02-02

  The present invention provides compounds of formula (I), and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2 and FGFR-1, thereby making them useful as anti-cancer agents. The formula (I) compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.

  本发明提供了式(I)化合物及其药学上可接受的盐类。式（I）化合物可抑制生长因子受体（如 VEGFR-2 和 FGFR-1）的酪氨酸激酶活性，因此可用作抗癌剂。式 (I) 化合物还可用于治疗与通过生长因子受体运行的信号转导通路有关的其他疾病。