泰地唑胺杂质35 | 1256966-02-5

• 物质功能分类: 分析化学 - 标准品 - 药典标准品和杂质标准品
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: 泰地唑胺杂质35
• 中文别名: 磷酸特地唑胺双磷酸酯；特地唑胺杂质37
• 英文名称: 2CZ2P66U2C
• 英文别名: bis[[(5R)-3-[3-fluoro-4-[6-(2-methyltetrazol-5-yl)pyridin-3-yl]phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl] hydrogen phosphate
• CAS: 1256966-02-5
• 化学式: C₃₄H₂₉F₂N₁₂O₈P
• 分子量: 802.65
• InChiKey: UGUGELYBSIMIPH-DNQXCXABSA-N

物化性质

• 沸点：
  989.4±75.0 °C(Predicted)
• 密度：
  1.70±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  57
• 可旋转键数：
  12
• 环数：
  8.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  228
• 氢给体数：
  1
• 氢受体数：
  18

反应信息

• 作为产物：
  描述：

  特地唑胺 在 三乙胺 、 三氯氧磷 作用下， 以 四氢呋喃 为溶剂， 反应 16.0h， 以20%的产率得到泰地唑胺杂质35
  参考文献：
  名称：

  [EN] OXAZOLIDINONE CONTAINING DIMER COMPOUNDS, COMPOSITIONS AND METHODS TO MAKE AND USE
  [FR] COMPOSÉS DIMÈRES CONTENANT DE L'OXAZOLIDINONE, COMPOSITIONS ET PROCÉDÉS DE FABRICATION ET D'UTILISATION

  摘要：

  药物剂型或制剂组合物包括具有公式（IV）结构的化合物，其中n是非负整数；其中每个Z是含氧杂环的基团，在裂解时具有体内抗生素活性，其中M独立地为OR1或NR1R2；其中R1和R2独立地选自H，可选取取代的烃基残基或药学上可接受的阳离子；其中剂型或制剂组合物中的化合物以有效量存在，用于治疗或预防哺乳动物主体的抗菌感染。还公开了制备和使用这些药物剂型或制剂组合物的方法。

  公开号：

  WO2010138649A1

文献信息

• Forms of R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate
  申请人：Merck Sharp & Dohme Corp.

  公开号：US10442829B2

  公开（公告）日：2019-10-15

  A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the crystalline form may be used in antibiotics.

  (R)-3-(4-(2-(2-甲基四唑-5-基)-吡啶-5-基)-3-氟苯基)-5-羟甲基噁唑烷-2-酮二氢磷酸酯的结晶形式、结晶形式的制造方法和包含结晶形式的药物组合物是有用的抗生素。此外，本发明的衍生物可对各种人类和动物病原体发挥强效抗菌活性，包括革兰氏阳性细菌（如葡萄球菌、肠球菌和链球菌）、厌氧微生物（如乳酸杆菌和梭状芽孢杆菌）以及耐酸微生物（如结核分枝杆菌和分枝杆菌）。因此，包含晶体的组合物可用于抗生素。
• CRYSTALLINE FORM OF R)-3-(4-(2-(2-METHYLTETRAZOL-5-YL)PYRIDIN-5-YL)-3-FLUOROPHENYL)-5-HYDROXYMETHYL OXAZOLIDIN-2-ONE DIHYDROGEN PHOSPHATE
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP2393808B1

  公开（公告）日：2019-05-08
• CRYSTALLINE FORM OF R)-3-(4-(2-(2-METHYLTETRAZOL-5-YL)PYRIDIN- 5-YL)-3-FLUOROPHENYL)-5-HYDROXYMETHYL OXAZOLIDIN-2-ONE DIHYDROGEN PHOSPHATE
  申请人：Reichenbächer Katharina

  公开号：US20100227839A1

  公开（公告）日：2010-09-09

  A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium . Accordingly, the compositions comprising the crystalline form may be used in antibiotics.
• FORMS OF R)-3-(4-(2-(2-METHYLTETRAZOL-5-YL)PYRIDIN-5-YL)-3-FLUOROPHENYL)-5-HYDROXYMETHYL OXAZOLIDIN-2-ONE DIHYDROGEN PHOSPHATE
  申请人：Merck Sharp & Dohme Corp.

  公开号：US20160176905A1

  公开（公告）日：2016-06-23

  A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi , anaerobic microorganisms such as Bacteroides and Clostridia , and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium . Accordingly, the compositions comprising the crystalline form may be used in antibiotics.
• US8426389B2
  申请人：——

  公开号：US8426389B2

  公开（公告）日：2013-04-23