1-{2-[3-Fluoro-6-(methoxy)-1,5-naphthyridin-4-yl]ethyl}-4-piperidinamine | 724788-72-1

• 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: 1-{2-[3-Fluoro-6-(methoxy)-1,5-naphthyridin-4-yl]ethyl}-4-piperidinamine
• 英文别名: 1-[2-(3-fluoro-6-methoxy-1,5-naphthyridin-4-yl)ethyl]piperidin-4-amine
• CAS: 724788-72-1
• 化学式: C₁₆H₂₁FN₄O
• 分子量: 304.367
• InChiKey: BQQUIDBKXSZWQL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  22
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  64.3
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  2,3-二氢[1,4]二恶并[2,3-c]吡啶-7-甲醛 、 1-{2-[3-Fluoro-6-(methoxy)-1,5-naphthyridin-4-yl]ethyl}-4-piperidinamine 以 甲醇 、 氯仿 为溶剂， 反应 4.0h， 生成
  参考文献：
  名称：

  Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases

  摘要：

  We have identified a series of amino-piperidine antibacterials with a good broad spectrum potency. We report the investigation of various subunits in this series and advanced studies on compound 8. Compound 8 possesses good pharmacokinetics, broad spectrum antibacterial activity and demonstrates oral efficacy in a rat lung infection model. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.09.117
• 作为产物：
  描述：

  7-fluoro-2-methoxy-8-vinyl-1,5-naphthyridine 在 N,N-二甲基甲酰胺 、 三氟乙酸 作用下， 反应 29.5h， 生成 1-{2-[3-Fluoro-6-(methoxy)-1,5-naphthyridin-4-yl]ethyl}-4-piperidinamine
  参考文献：
  名称：

  Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases

  摘要：

  We have identified a series of amino-piperidine antibacterials with a good broad spectrum potency. We report the investigation of various subunits in this series and advanced studies on compound 8. Compound 8 possesses good pharmacokinetics, broad spectrum antibacterial activity and demonstrates oral efficacy in a rat lung infection model. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.09.117

文献信息

• Antibacterial agents
  申请人：Axten MICHAEL Jeffrey

  公开号：US20060041123A1

  公开（公告）日：2006-02-23

  Quinoline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans.

  喹啉和萘啶衍生物可用于治疗哺乳动物（尤其是人类）的细菌感染。
• ANTIBACTERIAL AGENTS
  申请人：GLAXO GROUP LIMITED

  公开号：EP1578743A2

  公开（公告）日：2005-09-28
• EP1578743A4
  申请人：——

  公开号：EP1578743A4

  公开（公告）日：2006-11-29
• [EN] ANTIBACTERIAL AGENTS<br/>[FR] AGENTS ANTIBACTERIENS
  申请人：GLAXO GROUP LTD

  公开号：WO2004058144A2

  公开（公告）日：2004-07-15

  Quinoline and naphthyridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans.
• Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases
  作者：Timothy J. Miles、Jeffrey M. Axten、Christopher Barfoot、Gerald Brooks、Pamela Brown、Dongzhao Chen、Steven Dabbs、David T. Davies、David L. Downie、Susanne Eyrisch、Timothy Gallagher、Ilaria Giordano、Michael N. Gwynn、Alan Hennessy、Jennifer Hoover、Jianzhong Huang、Graham Jones、Roger Markwell、William H. Miller、Elizabeth A. Minthorn、Stephen Rittenhouse、Mark Seefeld、Neil Pearson

  DOI：10.1016/j.bmcl.2011.09.117

  日期：2011.12

  We have identified a series of amino-piperidine antibacterials with a good broad spectrum potency. We report the investigation of various subunits in this series and advanced studies on compound 8. Compound 8 possesses good pharmacokinetics, broad spectrum antibacterial activity and demonstrates oral efficacy in a rat lung infection model. (C) 2011 Elsevier Ltd. All rights reserved.