[(5R)-3-(3-fluoro-4-morpholin-4-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl 4-nitrobenzenesulfonate | 198410-26-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: [(5R)-3-(3-fluoro-4-morpholin-4-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl 4-nitrobenzenesulfonate
• CAS: 198410-26-3
• 化学式: C₂₀H₂₀FN₃O₈S
• 分子量: 481.459
• InChiKey: CBFVVHIQTUPBHR-MRXNPFEDSA-N

物化性质

• 沸点：
  686.8±55.0 °C(Predicted)
• 密度：
  1.483±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  33
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  140
• 氢给体数：
  0
• 氢受体数：
  10

反应信息

• 作为反应物：
  描述：

  [(5R)-3-(3-fluoro-4-morpholin-4-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl 4-nitrobenzenesulfonate 在 氨 作用下， 以 甲醇 为溶剂， 反应 2.0h， 生成 利奈唑胺
  参考文献：
  名称：

  Synthesis and antibacterial activity of linezolid analogues

  摘要：

  Several new compounds of oxazolidinone class were designed and synthesized referring to the structure-activity relationship studies and the synthesis of Linezolid, and their antibacterial activity was studied. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(02)00043-4
• 作为产物：
  描述：

  3,4-二氟硝基苯 在 palladium on activated charcoal 正丁基锂 、 ammonium formate 、 碳酸氢钠 、 三乙胺 、 N,N-二异丙基乙胺 作用下， 以 四氢呋喃 、 甲醇 、 正己烷 为溶剂， 生成 [(5R)-3-(3-fluoro-4-morpholin-4-ylphenyl)-2-oxo-1,3-oxazolidin-5-yl]methyl 4-nitrobenzenesulfonate
  参考文献：
  名称：

  Synthesis and antibacterial activity of linezolid analogues

  摘要：

  Several new compounds of oxazolidinone class were designed and synthesized referring to the structure-activity relationship studies and the synthesis of Linezolid, and their antibacterial activity was studied. (C) 2002 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(02)00043-4

文献信息

• IMPROVED PROCESSES FOR THE PREPARATION OF LINEZOLID USING NOVEL INTERMEDIATES
  申请人：SYMED LABS LIMITED

  公开号：US20160102064A1

  公开（公告）日：2016-04-14

  Provided herein are improved, commercially viable and industrially advantageous processes for the preparation of Linezolid, in high yield and purity, using novel intermediates. In one aspect, provided herein are efficient, industrially advantageous and environmentally friendly processes for the preparation of linezolid, in high yield and with high purity, using novel intermediates. The processes disclosed herein avoid the tedious and cumbersome procedures of the prior processes, thereby resolving the problems associated with the processes described in the prior art, which is more convenient to operate at lab scale and in commercial scale operations.

  本文提供了一种改进的、商业可行的、工业上优越的过程，用于使用新型中间体高产高纯度制备Linezolid。在一个方面，本文提供了一种高效、工业优越、环境友好的过程，用于使用新型中间体高产高纯度制备Linezolid。本文所披露的过程避免了先前过程的繁琐和麻烦程序，从而解决了与先前技术描述的过程相关的问题，更方便地在实验室规模和商业规模操作。
• US9586913B2
  申请人：——

  公开号：US9586913B2

  公开（公告）日：2017-03-07
• [EN] A PROCESS FOR THE PREPARATION OF (5S)-(N)-[[3-[3-FLUORO-4-(4-MORPHOLINYL) PHENYL]-2-OXO-5-OXAZOLIDINYL] METHYL] ACETAMIDE<br/>[FR] PROCÉDÉ DE PRÉPARATION DE (5S)-(N)-[[3-[3-FLUORO-4-(4-MORPHOLINYL)PHÉNYL]-2-OXO-5-OXAZOLIDINYL]MÉTHYL]ACÉTAMIDE
  申请人：NEULAND LAB LTD

  公开号：WO2010084514A2

  公开（公告）日：2010-07-29

  The present invention is directed to a novel, industrially viable, cost effective process for manufacturing (5S)-N-[[3-[3-Fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl] methyl] acetamide going through a novel intermediate of Formula XXI and XXII.
• Synthesis and antibacterial activity of linezolid analogues
  作者：Du Yu、Guo Huiyuan

  DOI：10.1016/s0960-894x(02)00043-4

  日期：2002.3

  Several new compounds of oxazolidinone class were designed and synthesized referring to the structure-activity relationship studies and the synthesis of Linezolid, and their antibacterial activity was studied. (C) 2002 Elsevier Science Ltd. All rights reserved.