(5R)-3-[4-(5,6-dihydro-1H-1,2,4-triazin-4-yl)-3-fluorophenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one | 1219707-38-6

• 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-[4-(5,6-dihydro-1H-1,2,4-triazin-4-yl)-3-fluorophenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one
• CAS: 1219707-38-6
• 化学式: C₁₃H₁₅FN₄O₃
• 分子量: 294.286
• InChiKey: ZNAHKJBWFGFEFA-SNVBAGLBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  77.4
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  (5R)-3-[4-(5,6-dihydro-1H-1,2,4-triazin-4-yl)-3-fluorophenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one 以45的产率得到德帕唑胺
  参考文献：
  名称：

  Oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone pharmaceutical compositions thereof

  摘要：

  本发明涉及一种新型的噁唑烷酮衍生物，特别是具有环状酰肟基或环状酰肼基的新型噁唑烷酮化合物。同时，本发明还涉及一种包括新型噁唑烷酮衍生物、体内可水解酯或体内可水解磷酸酯、其异构体或其药学上可接受的盐作为有效成分的制药抗生素组合物。由于新型噁唑烷酮衍生物、体内可水解酯或体内可水解磷酸酯、其异构体或其药学上可接受的盐对抗耐药菌具有广谱抗菌谱、低毒性和对革兰氏阳性和革兰氏阴性菌的强烈抗菌活性，因此可以作为一种有用的抗生素。

  公开号：

  US08242113B2
• 作为产物：
  描述：

  4-[2-fluoro-4-[(5R)-5-(hydroxymethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]-5,6-dihydro-1,2,4-triazine-1-carbaldehyde 以74的产率得到(5R)-3-[4-(5,6-dihydro-1H-1,2,4-triazin-4-yl)-3-fluorophenyl]-5-(hydroxymethyl)-1,3-oxazolidin-2-one
  参考文献：
  名称：

  Oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone pharmaceutical compositions thereof

  摘要：

  本发明涉及一种新型的噁唑烷酮衍生物，特别是具有环状酰肟基或环状酰肼基的新型噁唑烷酮化合物。同时，本发明还涉及一种包括新型噁唑烷酮衍生物、体内可水解酯或体内可水解磷酸酯、其异构体或其药学上可接受的盐作为有效成分的制药抗生素组合物。由于新型噁唑烷酮衍生物、体内可水解酯或体内可水解磷酸酯、其异构体或其药学上可接受的盐对抗耐药菌具有广谱抗菌谱、低毒性和对革兰氏阳性和革兰氏阴性菌的强烈抗菌活性，因此可以作为一种有用的抗生素。

  公开号：

  US08242113B2

文献信息

• [EN] NOVEL OXAZOLIDINONE DERIVATIVE HAVING CYCLIC AMIDRAZONE GROUP AND PHARMACEUTICAL COMPOSITION CONTAINING SAME<br/>[FR] NOUVEAU DÉRIVÉ D'OXAZOLIDINONE AYANT UN GROUPE AMIDRAZONE CYCLIQUE ET COMPOSITION PHARMACEUTIQUE LE CONTENANT
  申请人：LEGOCHEM BIOSCIENCES INC

  公开号：WO2012121424A1

  公开（公告）日：2012-09-13

  본 발명은 신규한 옥사졸리디논 유도체, 특히 사이클릭 아미드라존 기를 가지는 신규한 옥사졸리디논 화합물에 관한 것이다. 또한 본 발명은 신규한 옥사졸리디논 유도체, 이의 프로드럭, 이의 수화물, 이의 용매화물, 이의 이성질체 및 이의 약제학적으로 허용되는 염을 유효성분으로 함유하는 항생제용 의약 조성물에 관한 것이다. 본 발명에 따른 신규한 옥사졸리디논 유도체, 이의 프로드럭, 이의 수화물, 이의 용매화물, 이의 이성질체 및 이의 약제학적으로 허용되는 염은 내성균에 대한 항균 스펙트럼이 넓고, 독성이 낮으며, 그람양성 및 그람음성균에 강한 항균효과를 나타내므로, 항생제로 유용하게 사용될 수 있다.

  本发明涉及一种新型的氧唑啉衍生物，特别是具有环酰胺基的新型氧唑啉化合物。此外，本发明涉及一种含有新型氧唑啉衍生物、其前药、水合物、溶剂化合物、异构体以及药学上允许的盐作为有效成分的抗生素药物组合物。根据本发明的新型氧唑啉衍生物、其前药、水合物、溶剂化合物、异构体以及药学上允许的盐具有广泛的抗菌谱，低毒性，对革兰氏阳性和革兰氏阴性菌具有强烈的抗菌效果，因此可以作为一种有用的抗生素。
• [EN] NOVEL OXAZOLIDINONE DERIVATIVES WITH CYCLIC AMIDOXIME OR CYCLIC AMIDRAZONE AND PHARMACEUTICAL COMPOSITIONS THEREOF<br/>[FR] NOUVEAUX DÉRIVÉS D'OXAZOLIDINONE AVEC UNE AMIDOXIME CYCLIQUE OU UNE AMIDRAZONE CYCLIQUE ET COMPOSITIONS PHARMACEUTIQUES LES COMPRENANT
  申请人：LEGOCHEM BIOSCIENCE LTD

  公开号：WO2010036000A3

  公开（公告）日：2010-07-15
• Novel Oxazolidinone Derivatives with Cyclic Amidoxime or Cyclic Amidrazone and Pharmaceutical Compositions Thereof
  申请人：Cho Young Lag

  公开号：US20110178293A1

  公开（公告）日：2011-07-21

  Disclosed is a novel oxazolidinone derivative, particularly a novel oxazolidinone compound with a cyclic amidoxime or cyclic amidrazone group. Also disclosed is a pharmaceutical antibiotic composition including a novel oxazolidinone derivative, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof or a pharmaceutically acceptable salt thereof as an effective ingredient. Because the novel oxazolidinone derivative, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof or a pharmaceutically acceptable salt thereof exhibits a wide antibacterial spectrum against resistant bacteria, a low toxicity, and a strong antibacterial activity against Gram-positive and Gram-negative bacteria, it can be usefully used as an antibiotic.
• US8242113B2
  申请人：——

  公开号：US8242113B2

  公开（公告）日：2012-08-14
• Oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone pharmaceutical compositions thereof
  申请人：Legochem Biosciences, Inc.

  公开号：US08242113B2

  公开（公告）日：2012-08-14

  Disclosed is a novel oxazolidinone derivative, particularly a novel oxazolidinone compound with a cyclic amidoxime or cyclic amidrazone group. Also disclosed is a pharmaceutical antibiotic composition including a novel oxazolidinone derivative, in vivo hydrolysable ester thereof, in vivo hydrolysable phosphate ester thereof, an isomer thereof or a pharmaceutically acceptable salt thereof as an effective ingredient. Because the novel oxazolidinone derivative, in vivo hydrolysable ester thereof, in vivo hydrolysable phosphate ester thereof, an isomer thereof or a pharmaceutically acceptable salt thereof exhibits a wide antibacterial spectrum against resistant bacteria, a low toxicity, and a strong antibacterial activity against Gram-positive and Gram-negative bacteria, it can be usefully used as an antibiotic.

  本发明涉及一种新型的噁唑烷酮衍生物，特别是具有环状酰肟基或环状酰肼基的新型噁唑烷酮化合物。同时，本发明还涉及一种包括新型噁唑烷酮衍生物、体内可水解酯或体内可水解磷酸酯、其异构体或其药学上可接受的盐作为有效成分的制药抗生素组合物。由于新型噁唑烷酮衍生物、体内可水解酯或体内可水解磷酸酯、其异构体或其药学上可接受的盐对抗耐药菌具有广谱抗菌谱、低毒性和对革兰氏阳性和革兰氏阴性菌的强烈抗菌活性，因此可以作为一种有用的抗生素。