O-[5-(4-aminothiazol-2-yl)-pyridin-2-ylmethyl]-hydroxylamine | 1127403-20-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: O-[5-(4-aminothiazol-2-yl)-pyridin-2-ylmethyl]-hydroxylamine
• 英文别名: O-[[5-(4-amino-1,3-thiazol-2-yl)pyridin-2-yl]methyl]hydroxylamine
• CAS: 1127403-20-6
• 化学式: C₉H₁₀N₄OS
• 分子量: 222.271
• InChiKey: SBEPYMNPQFGOTR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  115
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  O-[5-(4-aminothiazol-2-yl)-pyridin-2-ylmethyl]-hydroxylamine 在 盐酸 、 甲醇 作用下， 以 乙醇 、 水 为溶剂， 反应 32.0h， 生成 C₄₄H₆₅FN₆O₁₁S
  参考文献：
  名称：

  [EN] 6,11-BICYCLOLIDES: BRIDGED BIARYL AMIDE MACROLIDE DERIVATIVES
  [FR] 6,11-BICYCLOLIDES : DÉRIVÉS DE BIARYLE AMIDE MACROLIDE PONTÉS

  摘要：

  本发明公开了化合物I和II及其在体内表现出抗菌特性的药用盐。本发明还涉及包含上述化合物的药物组合物，用于给需要抗生素治疗的受试者使用。该发明还涉及通过给予包含本发明化合物的药物组合物来治疗受试者的细菌感染的方法。该发明还包括制备本发明化合物的方法。

  公开号：

  WO2010096051A1

文献信息

• 6,11-BICYCLOLIDES: BRIDGED BIARYL MACROLIDE DERIVATIVES
  申请人：KIM IN JONG

  公开号：US20090075915A1

  公开（公告）日：2009-03-19

  The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

  本发明揭示了以下化合物的化学式I，或其药学上可接受的盐、酯或前药：这些化合物具有抗菌性能。本发明还涉及包含上述化合物的药物组合物，用于治疗需要抗生素治疗的患者。该发明还涉及通过给予含有本发明化合物的药物组合物来治疗患者的细菌感染的方法。该发明还包括制备本发明化合物的方法。
• ANTI-BACTERIAL ACTIVITY OF 9-HYDROXY DERIVATIVES OF 6,11-BICYCLOLIDES
  申请人：Iyengar Rajesh

  公开号：US20090281050A1

  公开（公告）日：2009-11-12

  The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit superior antibacterial properties, particularly against Haemophilus influenzae . The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.

  本发明揭示了具有以下式（I）的化合物或其药学上可接受的盐、酯或前药：这些化合物表现出优越的抗菌特性，特别是对Haemophilus influenzae。本发明还涉及包含上述化合物的药物组合物，用于给需要抗生素治疗的受试者进行治疗。该发明还涉及通过给予包含本发明化合物的药物组合物来治疗受试者的细菌感染的方法。该发明还包括制备本发明化合物的方法。
• PROCESSES FOR THE PREPARATION OF 2 FLUORO 6-11 BICYCLIC ERYTHROMYCIN DERIVATIVES
  申请人：Xu Guoyou

  公开号：US20090281293A1

  公开（公告）日：2009-11-12

  The present invention relates to processes and intermediates for the preparation of 2-fluoro 6-11 bicyclic erythromycin derivatives. In particular, the present invention relates to processes and intermediates for the preparation of a compound of formula (X-c):

  本发明涉及用于制备2-氟-6-11环状红霉素衍生物的过程和中间体。特别地，本发明涉及用于制备式（X-c）化合物的过程和中间体。
• PROCESSES FOR THE PREPARATION OF O-[5-(4-AMINO-THIAZOL-2-YL)-PYRIDIN-2-YLMETHYL]-HYDROXYLAMINE
  申请人：Tang Datong

  公开号：US20090281324A1

  公开（公告）日：2009-11-12

  The present invention relates generally to novel methods for the synthesis of O-[5-(4-amino-thiazol-2-yl)-pyridin-2-ylmethyl]-hydroxylamine which is an essential reagent in the synthesis of one of the bridged erythromycin derivatives and their respective pharmaceutically acceptable salts in PCT Application WO 03/097659 A1. In particular, the present invention relates to processes and intermediates for the preparation of a compound of formula (Ia):

  本发明涉及一种新颖的合成O-[5-(4-氨基噻唑-2-基)-吡啶-2-基甲基]-羟胺的方法，该化合物是桥接红霉素衍生物及其相应的药学上可接受的盐合成中的重要试剂，其在PCT申请WO 03/097659 A1中描述。具体而言，本发明涉及制备式(Ia)化合物的过程和中间体：
• PROCESSES FOR THE PREPARATION OF 2-FLUORO 6-11 BICYCLIC ERYTHROMYCIN DERIVATIVES
  申请人：Enanta Pharmaceuticals, Inc.

  公开号：US20140073797A1

  公开（公告）日：2014-03-13

  The present invention relates to processes and intermediates for the preparation of 2-fluoro 6-11 bicyclic erythromycin derivatives. In particular, the present invention relates to processes and intermediates for the preparation of a compound of formula (X-c):

  本发明涉及用于制备2-氟-6-11环状红霉素衍生物的过程和中间体。特别地，本发明涉及用于制备化合物（X-c）的过程和中间体。