D-(-)-threo-2-phenyl-4-(fluoromethyl)-5-[4-(methylsulfonyl)phenyl]-2-oxazoline

• 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: D-(-)-threo-2-phenyl-4-(fluoromethyl)-5-[4-(methylsulfonyl)phenyl]-2-oxazoline
• 英文别名: (4S,5R)-4-(Fluoromethyl)-4,5-dihydro-5-[4-(methylsulfonyl)phenyl]-2-phenyl-oxazole-d3；4-(fluoromethyl)-5-(4-methylsulfonylphenyl)-2-phenyl-4,5-dihydro-1,3-oxazole
• 化学式: C₁₇H₁₆FNO₃S
• 分子量: 333.383
• InChiKey: AMZCJDBNQOWJJF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  64.1
• 氢给体数：
  0
• 氢受体数：
  5

文献信息

• Process for the synthesis of intermediates of chloramphenicol or its analogues
  申请人：KRKA, tovarna zdravil, d.d., Novo mesto

  公开号：EP1785414A1

  公开（公告）日：2007-05-16

  The present invention relates to the synthesis of antibacterial compounds such as Chloramphenicol and its analogues Thiamphenicol and Florfenicol and particularly to a new reaction for the preparation of the intermediate compound aminodiolphenylsulfone. This reaction permits the introduction of modified residues to obtain modified antibiotics with an improved stability towards the action of bacterial resistant determinants. In addition, higher purities may be also obtained due to an improved procedure requiring fewer purification steps.

  本发明涉及抗菌化合物的合成，如氯霉素及其类似物硫胺苯酚和氟苯胺，特别涉及一种用于制备中间体氨基二酚苯砜的新反应。该反应允许引入修饰残基，以获得对细菌耐药基因作用具有改进稳定性的修饰抗生素。此外，由于改进的程序需要更少的纯化步骤，也可以获得更高的纯度。
• Fluorination process
  申请人：SCHERING CORPORATION

  公开号：EP0359190A1

  公开（公告）日：1990-03-21

  There is disclosed a high yielding process for converting a hydroxy compound to the corresponding fluoro derivative by reacting the hydroxy compound with α, α-­difluoroalkylamine under pressure.

  本发明公开了一种高产工艺，通过羟基化合物与 α, α-二氟烷基胺在压力下反应，将羟基化合物转化为相应的氟衍生物。
• Intermediates for the preparation of 1-(phenyl)-1-hydroxy-2-amino-3-fluoro propane derivatives
  申请人：ZAMBON GROUP S.p.A.

  公开号：EP0678506A2

  公开（公告）日：1995-10-25

  A process for preparing a D-threo compound of the formula wherein R, and R1 have the meanings shown in the description, via protection of both the secondary hydroxy and the amino group of a corresponding D-threo 1-(phenyl)-2-amino-1,3-propanediol, fluorination of the protected compound and treatment of the thus obtained compound to afford a D-threo compound of the formula (II).

  一种制备式 D-硫代化合物的工艺 其中 R 和 R1 具有说明中所示的含义，通过保护相应 D-硫代 1-(苯基)-2-氨基-1,3-丙二醇的仲羟基和氨基，将保护后的化合物氟化，并处理由此得到的化合物，得到式 (II) 的 D-硫代化合物。
• Process for the preparation of 1-(phenyl)-1-hydroxy-2-amino-3-fluoro propane derivatives
  申请人：ZAMBON GROUP S.p.A.

  公开号：EP0130633B1

  公开（公告）日：1996-10-09
• IMPROVED FLUORINATION PROCESS
  申请人：SCHERING CORPORATION

  公开号：EP0434732A1

  公开（公告）日：1991-07-03