5(R)-azidomethyl-3-[4-(1-cyanocyclopropan-1-yl)-3-fluorophenyl]oxazolidin-2-one | 543683-29-0

• 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: 5(R)-azidomethyl-3-[4-(1-cyanocyclopropan-1-yl)-3-fluorophenyl]oxazolidin-2-one
• 英文别名: 1-[4-[(5R)-5-(azidomethyl)-2-oxo-1,3-oxazolidin-3-yl]-2-fluorophenyl]cyclopropane-1-carbonitrile
• CAS: 543683-29-0
• 化学式: C₁₄H₁₂FN₅O₂
• 分子量: 301.28
• InChiKey: XBZJONODBJFDRA-JTQLQIEISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  22
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  67.7
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  5(R)-azidomethyl-3-[4-(1-cyanocyclopropan-1-yl)-3-fluorophenyl]oxazolidin-2-one 在 Lindlars catalyst 作用下， 以 甲醇 为溶剂， 25.0 ℃ 、13.51 MPa 条件下， 反应 3.0h， 以to give 5(S)-aminomethyl-3-[4-(1-cyanocyclopropan-1-yl)-3-fluorophenyl]oxazolidin-2-one的产率得到5(S)-aminomethyl-3-[4-(1-cyanocyclopropan-1-yl)-3-fluorophenyl]oxazolidin-2-one
  参考文献：
  名称：

  CYCLOPROPYL CONTAINING OXAZOLIDINONE ANTIBIOTICS AND DERIVATIVES THEREOF

  摘要：

  本发明涉及一种具有环丙基基团的新型噁唑烷酮，对包括多重耐药葡萄球菌、链球菌和肠球菌、Bacteroides spp.、Clostridia spp. 等厌氧和需氧病原体以及酸性快速生物如结核分枝杆菌和其他分枝杆菌等具有有效作用。该化合物由结构式I表示：1，其对映异构体、顺异构体或其药学上可接受的盐或酯。

  公开号：

  US20030225107A1

文献信息

• CYCLOPROPYL CONTAINING OXAZOLIDINONE ANTIBIOTICS AND DERIVATIVES THEREOF
  申请人：——

  公开号：US20030225107A1

  公开（公告）日：2003-12-04

  This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: 1 its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.

  这项发明涉及新的含有环丙基基团的噁唑烷酮类化合物，这些化合物对包括多耐药葡萄球菌、链球菌和肠球菌、拟杆菌属、梭菌属等好氧菌和厌氧菌，以及结核分枝杆菌和其他分枝杆菌属等抗酸菌有效。这些化合物由结构式I表示：1其对应的手性异构体、对映异构体或药用可接受的盐或酯。
• CYCLOPROPYL-CONTAINING OXAZOLIDINONE ANTIBIOTICS AND DERIVATIVES THEREOF
  申请人：Merck & Co., Inc.

  公开号：EP1448536A1

  公开（公告）日：2004-08-25
• US6686363B2
  申请人：——

  公开号：US6686363B2

  公开（公告）日：2004-02-03
• [EN] CYCLOPROPYL HEXANE CONTAINING OXAZOLIDINONE ANTIBIOTICS AND DERIVATIVES THEREOF<br/>[FR] ANTIBIOTIQUES DE TYPE OXAZOLIDINONE CONTENANT DE L'HEXANE CYCLOPROPYLE ET DERIVES DE CEUX-CI
  申请人：MERCK & CO INC

  公开号：WO2003048136A1

  公开（公告）日：2003-06-12

  This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula (I): its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.
• Cyclopropyl containing oxazolidinone antibiotics and derivatives thereof
  申请人：Kyorin Pharmaceutical Co., Ltd.

  公开号：US06686363B2

  公开（公告）日：2004-02-03

  This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.

  本发明涉及新的含环丙基基团的噁唑烷酮化合物，对于厌氧和需氧病原体如多重耐药葡萄球菌、链球菌和肠球菌、Bacteroides spp.、Clostridia spp.以及酸性快速细菌如结核分枝杆菌和其他分枝杆菌有良好的疗效。该化合物由结构式I表示：其对映异构体、顺反异构体或药学上可接受的盐或酯。