Ethyl 4-[7-methoxy-5-(trifluoromethyl)-1,8-naphthyridin-2-yl]piperazine-1-carboxylate | 210643-02-0

• 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: Ethyl 4-[7-methoxy-5-(trifluoromethyl)-1,8-naphthyridin-2-yl]piperazine-1-carboxylate
• CAS: 210643-02-0
• 化学式: C₁₇H₁₉F₃N₄O₃
• 分子量: 384.358
• InChiKey: JRNYPLQHCKRLCH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  67.8
• 氢给体数：
  0
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  Ethyl 4-[7-methoxy-5-(trifluoromethyl)-1,8-naphthyridin-2-yl]piperazine-1-carboxylate 在 sodium hydroxide 作用下， 以 甲醇 为溶剂， 反应 8.0h， 以80%的产率得到2-Methoxy-7-piperazin-1-yl-4-(trifluoromethyl)-1,8-naphthyridine
  参考文献：
  名称：

  Synthesis of 1,8-naphthyridine derivatives: Potential antihypertensive agents — Part VII

  摘要：

  A series of 2-(carbethoxypiperazinyl)- and 2-piperazinyl-1,8-naphthyridine derivatives, variously substituted, have been synthesized and pharmacologically investigated for their antihypertensive activity. Some of them exhibited a significant and prolonged decrease of the mean arterial pressure (MAP) on spontaneously hypertensive rats. For this series of compounds, on the basis of the pharmacological results obtained, no structure-activity relationship can be deduced at this time. Moreover, the most active and representative compounds 11b, 12a and 16b were investigated by means of in vitro pharmacological functional studies and in vivo, as diuretic agents, to determine a possible mechanism of the antihypertensive activity, which is unknown for the moment. (C) Elsevier, Paris.

  DOI：

  10.1016/s0223-5234(98)80014-7
• 作为产物：
  描述：

  2,6-二氨基吡啶 在 ammonium hydroxide 、 硫酸 、 三乙胺 、 sodium nitrite 、 三氯氧磷 作用下， 以 甲醇 为溶剂， 反应 70.0h， 生成 Ethyl 4-[7-methoxy-5-(trifluoromethyl)-1,8-naphthyridin-2-yl]piperazine-1-carboxylate
  参考文献：
  名称：

  Synthesis of 1,8-naphthyridine derivatives: Potential antihypertensive agents — Part VII

  摘要：

  A series of 2-(carbethoxypiperazinyl)- and 2-piperazinyl-1,8-naphthyridine derivatives, variously substituted, have been synthesized and pharmacologically investigated for their antihypertensive activity. Some of them exhibited a significant and prolonged decrease of the mean arterial pressure (MAP) on spontaneously hypertensive rats. For this series of compounds, on the basis of the pharmacological results obtained, no structure-activity relationship can be deduced at this time. Moreover, the most active and representative compounds 11b, 12a and 16b were investigated by means of in vitro pharmacological functional studies and in vivo, as diuretic agents, to determine a possible mechanism of the antihypertensive activity, which is unknown for the moment. (C) Elsevier, Paris.

  DOI：

  10.1016/s0223-5234(98)80014-7

文献信息

• Synthesis of 1,8-naphthyridine derivatives: Potential antihypertensive agents — Part VII
  作者：Pier Luigi Ferrarini、Claudio Mori、Muwaffag Badawneh、Vincenzo Calderone、Lorella Calzolari、Tiziana Loffredo、Enrica Martinotti、Giuseppe Saccomanni

  DOI：10.1016/s0223-5234(98)80014-7

  日期：1998.6

  A series of 2-(carbethoxypiperazinyl)- and 2-piperazinyl-1,8-naphthyridine derivatives, variously substituted, have been synthesized and pharmacologically investigated for their antihypertensive activity. Some of them exhibited a significant and prolonged decrease of the mean arterial pressure (MAP) on spontaneously hypertensive rats. For this series of compounds, on the basis of the pharmacological results obtained, no structure-activity relationship can be deduced at this time. Moreover, the most active and representative compounds 11b, 12a and 16b were investigated by means of in vitro pharmacological functional studies and in vivo, as diuretic agents, to determine a possible mechanism of the antihypertensive activity, which is unknown for the moment. (C) Elsevier, Paris.