(1RS,5S)-N-{3-[4-(1-cyano-6-aza-spiro[2.5]oct-6-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (1RS,5S)-N-{3-[4-(1-cyano-6-aza-spiro[2.5]oct-6-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide
• 英文别名: N-[[(5S)-3-[4-(2-cyano-6-azaspiro[2.5]octan-6-yl)-3-fluorophenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]acetamide
• 化学式: C₂₀H₂₃FN₄O₃
• 分子量: 386.426
• InChiKey: AFZFYXJGJDXKBA-WMCAAGNKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  28
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  85.7
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  (1RS,5S)-N-{3-[4-(1-cyano-6-aza-spiro[2.5]oct-6-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide 以 甲醇 、 异丙醇 为溶剂， 反应 1.0h， 生成 (1R,5S)-N-{3-[4-(1-cyano-6-aza-spiro[2.5]oct-6-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide 、 (1S,5S)-N-{3-[4-(1-cyano-6-aza-spiro[2.5]oct-6-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide
  参考文献：
  名称：

  [EN] SUBSTITUTED PIPERIDINO PHENYLOXAZOLIDINONES HAVING ANTIMICRIOBIAL ACTIVITY WITH IMPROVED IN VIVO EFFICACY
  [FR] PIPERIDINO PHENYLOXAZOLIDINONES SUBSTITUEES DONT L'ACTIVITE ANTIMICROBIENNE A UN MEILLEUR RENDEMENT IN VIVO

  摘要：

  公开号：

  WO2005054234A3
• 作为产物：
  描述：

  三甲基碘化亚砜 、 (S)-N-{3-[4-(4-cyanomethylidene-piperidin-1-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide 在 potassium tert-butylate 作用下， 以 二甲基亚砜 为溶剂， 以57%的产率得到(1RS,5S)-N-{3-[4-(1-cyano-6-aza-spiro[2.5]oct-6-yl)-3-fluorophenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide
  参考文献：
  名称：

  [EN] SUBSTITUTED PIPERIDINO PHENYLOXAZOLIDINONES HAVING ANTIMICRIOBIAL ACTIVITY WITH IMPROVED IN VIVO EFFICACY
  [FR] PIPERIDINO PHENYLOXAZOLIDINONES SUBSTITUEES DONT L'ACTIVITE ANTIMICROBIENNE A UN MEILLEUR RENDEMENT IN VIVO

  摘要：

  公开号：

  WO2005054234A3

文献信息

• Substituted piperidino phenyloxazolidinones having antimicrobial activity with improved in vivo efficacy
  申请人：Deshpande Keshav Prasad

  公开号：US20050143421A1

  公开（公告）日：2005-06-30

  The present invention provides agents having antimicrobial activity for preventing and treating infectious diseases. Thus, the present invention provides novel substituted piperidino phenyloxazolidinone derivatives, processes for making compounds as well as antimicrobial compositions containing said derivatives as active ingredients and methods of treating bacterial infections with the said derivatives.

  本发明提供了具有抗微生物活性的药剂，用于预防和治疗传染病。因此，本发明提供了新型的取代哌啶基苯并噁唑啉衍生物，制备该类化合物的方法，以及包含上述衍生物作为活性成分的抗微生物组合物和使用该类衍生物治疗细菌感染的方法。
• SUBSTITUTED PIPERIDINO PHENYLOXAZOLIDINONES HAVING ANTIMICROBIAL ACTIVITY WITH IMPROVED IN VIVO EFFICACY
  申请人：Deshpande Prasad Keshav

  公开号：US20100144735A1

  公开（公告）日：2010-06-10

  The present invention provides agents having antimicrobial activity for preventing and treating infectious diseases. Thus, the present invention provides novel substituted piperidino phenyloxazolidinone derivatives, processes for making compounds as well as antimicrobial compositions containing said derivatives as active ingredients and methods of treating bacterial infections with the said derivatives.

  本发明提供具有抗微生物活性的药剂，用于预防和治疗传染病。因此，本发明提供了新型的取代的哌啶基苯并噁唑啉衍生物，制备该化合物的方法以及含有该衍生物作为活性成分的抗微生物组合物和使用该衍生物治疗细菌感染的方法。
• SUBSTITUTED PIPERIDINO PHENYLOXAZOLIDINONES HAVING ANTIMICRIOBIAL ACTIVITY WITH IMPROVED I IN VIVO /I EFFICACY
  申请人：Wockhardt Limited

  公开号：EP1664038A2

  公开（公告）日：2006-06-07
• US7687627B2
  申请人：——

  公开号：US7687627B2

  公开（公告）日：2010-03-30
• US8729269B2
  申请人：——

  公开号：US8729269B2

  公开（公告）日：2014-05-20