5-ethyl-1,6-naphthyridin-2(1H)-one | 88877-10-5

• 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: 5-ethyl-1,6-naphthyridin-2(1H)-one
• 英文别名: 5-ethyl-1H-1,6-naphthyridin-2-one
• CAS: 88877-10-5
• 化学式: C₁₀H₁₀N₂O
• 分子量: 174.202
• InChiKey: IFXSSJQOSYDWES-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  42
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  5-amino-4-hexen-3-one 在 乙酸铵 、 Bredereck 试剂 作用下， 以 1,4-二氧六环 、 N,N-二甲基甲酰胺 为溶剂， 反应 32.0h， 生成 5-ethyl-1,6-naphthyridin-2(1H)-one
  参考文献：
  名称：

  Singh, Baldev; Lesher, George Y., Journal of Heterocyclic Chemistry, 1990, vol. 27, # 7, p. 2085 - 2091

  摘要：

  DOI：

文献信息

• Certain 2-(1H)-pyridinones cardiotonic compositions containing same and
  申请人：Sterling Drug Inc.

  公开号：US04415580A1

  公开（公告）日：1983-11-15

  1-R"-3-Q-4-R'-5-R-1,6-naphthyridin-2(1H)-ones (I) or salts thereof, where R is lower-alkyl, R' is hydrogen or methyl, R" is hydrogen or lower-alkyl, and Q is hydrogen, hydroxy, amino, cyano, carbamyl, carboxy or aminocarbamyl, are useful as cardiotonic agents (I, Q is hydrogen, hydroxy, amino, cyano or carbamyl) and/or intermediates therefor (I, Q is carboxy, aminocarbamyl, hydrogen, amino, cyano or carbamyl). Also shown are 3-Q"-4-R'-5-(RCO)-6-[2-(di-lower-alkylamino)ethenyl]-2(1H)-pyridinones (II) or salts thereof, where R and R' are as above and Q' is hydrogen or cyano, which are useful as cardiotonics (II, Q' is hydrogen) and/or intermediates (II, Q' is cyano or hydrogen). Processes for preparing the compounds of formulas I and II are shown.

  1-R"-3-Q-4-R'-5-R-1,6-萘啶并[2(1H)-酮]（I）或其盐，其中R为低碳烷基，R'为氢或甲基，R"为氢或低碳烷基，Q为氢、羟基、氨基、氰基、氨基甲酰基、羧基或氨基甲酰基，可用作强心药剂（I，Q为氢、羟基、氨基、氰基或氨基甲酰基）和/或其中间体（I，Q为羧基、氨基甲酰基、氢、氨基、氰基或氨基甲酰基）。还显示了3-Q"-4-R'-5-(RCO)-6-[2-(二低碳烷基氨基)乙烯基]-2(1H)-吡啶酮（II）或其盐，其中R和R'如上所述，Q'为氢或氰基，可用作强心剂（II，Q'为氢）和/或其中间体（II，Q'为氰基或氢）。显示了制备式I和II化合物的方法。
• 5-Alkyl-1,6-naphthyridin-2(1H)-ones and cardiotonic use thereof
  申请人：Sterling Drug Inc.

  公开号：US04517190A1

  公开（公告）日：1985-05-14

  1-R"-3-Q-4-R'-5-R-1,6-naphthyridin-2(1H)-ones (I) or salts thereof, where R is lower-alkyl, R' is hydrogen or methyl, R" is hydrogen or lower-alkyl, and Q is hydrogen, hydroxy, amino, cyano, carbamyl, carboxy or aminocarbamyl, are useful as cardiotonic agents (I, Q is hydrogen, hydroxy, amino, cyano or carbamyl) and/or intermediates therefor (I, Q is carboxy, aminocarbamyl, hydrogen, amino, cyano or carbamyl). Also shown are 3-Q'-4-R'-5-(RCO)-6-[2-(di-lower-alkylamino)ethenyl]-2(1H)-pyridinones (II) or salts thereof, where R and R' are as above and Q' is hydrogen or cyano, which are useful as cardiotonics (II, Q' is hydrogen) and/or intermediates (II, Q' is cyano or hydrogen). Processes for preparing the compounds of formulas I and II are shown.

  1-R"-3-Q-4-R'-5-R-1,6-萘啉并吡啶-2(1H)-酮(I)或其盐，其中R为较低烷基，R'为氢或甲基，R"为氢或较低烷基，Q为氢、羟基、氨基、氰基、氨基甲酰基、羧基或氨基甲酰基，可用作强心药剂(I，Q为氢、羟基、氨基、氰基或氨基甲酰基)和/或其中间体(I，Q为羧基、氨基甲酰基、氢、氨基、氰基或氨基甲酰基)。还显示了3-Q'-4-R'-5-(RCO)-6-[2-(二次较低烷基氨基)乙烯基]-2(1H)-吡啶酮(II)或其盐，其中R和R'如上所述，Q'为氢或氰基，可用作强心剂(II，Q'为氢)和/或中间体(II，Q'为氰基或氢)。显示了制备式I和II化合物的方法。
• 3-Substituted-5-alkyl-1,6-naphthyridin-2(1H)-ones, cardiotonic use and
  申请人：Sterling Drug Inc.

  公开号：US04559347A1

  公开（公告）日：1985-12-17

  1-R"-3-Q-4-R'-5-R-1,6-naphthyridin-2(1H)-ones (I) or salts thereof, where R is lower-alkyl, R' is hydrogen or methyl, R" is hydrogen or lower-alkyl, and Q is hydrogen, hydroxy, amino, cyano, carbamyl, carboxy or aminocarbamyl, are useful as cardiotonic agents (I, Q is hydrogen, hydroxy, amino, cyano or carbamyl) and/or intermediates therefor (I, Q is carboxy, aminocarbamyl, hydrogen, amino, cyano or carbamyl). Also shown are 3-Q'-4-R'-5-(RCO)-6-[2-di-lower-alkylamino)ethenyl]-2(1H)-pyridinones (II) or salts thereof, where R and R' are as above and Q' is hydrogen or cyano, which are useful as cardiotonics (II, Q' is hydrogen) and/or intermediates (II, Q' is cyano or hydrogen). Processes for preparing the compounds of formulas I and II are shown.

  1-R"-3-Q-4-R'-5-R-1,6-萘啶-2(1H)-酮(I)或其盐，其中R是低碳基，R'是氢或甲基，R"是氢或低碳基，Q是氢、羟基、氨基、氰基、氨基甲酰基、羧基或氨基甲酰基，可用作心力衰竭药物（I，Q为氢、羟基、氨基、氰基或氨基甲酰基）和/或其中间体（I，Q为羧基、氨基甲酰基、氢、氨基、氰基或氨基甲酰基）。还显示了3-Q'-4-R'-5-(RCO)-6-[2-二-低碳基氨基)乙烯基]-2(1H)-吡啶酮(II)或其盐，其中R和R'如上所述，Q'是氢或氰基，可用作心力衰竭药物（II，Q'为氢）和/或其中间体（II，Q'为氰基或氢）。显示了制备式I和式II化合物的方法。
• SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
  申请人：Rigel Pharmaceuticals, Inc.

  公开号：US20150072959A1

  公开（公告）日：2015-03-12

  Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.

  本文揭示了替代三唑类化合物及含有该化合物的药物组合物，用于抑制受体蛋白酪氨酸激酶Axl的活性。还揭示了使用该化合物治疗与Axl活性相关的疾病或病状的方法。
• 5-Alkyl-1,6-naphthyridin-2(1H)-ones, intermediates, their preparation and their cardiotonic use
  申请人：STERLING DRUG INC.

  公开号：EP0101952A1

  公开（公告）日：1984-03-07

  Naphthyridines of formula (I) , where R is -alkyl, R' is hydrogen or methyl, R" is hydrogen or alkyl, and Q is hydrogen, hydroxy, amino, cyano, carbamyl, carboxy or aminocarbamyl, are useful as cardiotonic agents (1, Q is hydrogen, hydroxy, amino, cyano or carbamyl) and/or intermediates therefor (I, Q is carboxy, aminocarbamyl, hydrogen, amino, cyano or carbamyl). Also shown are pyridinones of formula II where R and R' are as above and Q' is hydrogen or cyano, which are useful as cardiotonics (II, Q' is hydrogen) and/or intermediates (II, Q' is cyano or hydrogen). Processes for preparing the compounds of Formulas I and II are shown.

  式(I)的萘啶类化合物 其中 R 为烷基，R'为氢或甲基，R "为氢或烷基，Q 为氢、羟基、氨基、氰基、氨甲酰、羧基或氨基甲酰，可用作强心剂（1，Q 为氢、羟基、氨基、氰基或氨基甲酰）和/或其中间体（I，Q 为羧基、氨基甲酰、氢、氨基、氰基或氨基甲酰）。图中还显示了式 II 的吡啶酮类化合物 其中 R 和 R'如上，Q'为氢或氰基，可用作强心剂（II，Q'为氢）和/或中间体（II，Q'为氰基或氢）。所示为制备式 I 和 II 化合物的工艺。