methyl-2,6,7-tridesoxy-2,4-di-C-methyl-3,4-di-O-benzyl-α-D-glucoheptapyranoside | 81099-74-3

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: methyl-2,6,7-tridesoxy-2,4-di-C-methyl-3,4-di-O-benzyl-α-D-glucoheptapyranoside
• 英文别名: methyl 2,4-didesoxy-2,4,6-tri-C-methyl-3,4-di-O-benzyl-α-D-glucopyranoside；erythronolide A；(2R,3R,4R,5R,6S)-2-ethyl-6-methoxy-3,5-dimethyl-3,4-bis(phenylmethoxy)oxane
• CAS: 81099-74-3
• 化学式: C₂₄H₃₂O₄
• 分子量: 384.516
• InChiKey: SVRFSCJKFFCOFA-XNZCMHNBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  28
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  36.9
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  1,6-脱水-β-D-葡萄糖 在 盐酸 、 lithium aluminium tetrahydride 、 草酰氯 、 sodium hydride 、 三乙胺 、 间氯过氧苯甲酸 作用下， 以 四氢呋喃 、 乙醚 、 二氯甲烷 、 氯仿 、 二甲基亚砜 、 N,N-二甲基甲酰胺 、 苯 为溶剂， 反应 24.0h， 生成 methyl-2,6,7-tridesoxy-2,4-di-C-methyl-3,4-di-O-benzyl-α-D-glucoheptapyranoside
  参考文献：
  名称：

  Synthesis of macrolide antibiotics. 3. Revised synthesis of C9- C13 segment of erythronolide A.

  摘要：

  DOI：

  10.1016/s0040-4039(01)90023-1

文献信息

• Novel bicyclic 9a-azalide derivatives
  申请人：Or Sun Yat

  公开号：US20060069048A1

  公开（公告）日：2006-03-30

  The present invention discloses compounds of formulae I and II, 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.

  本发明公开了具有以下式I和II的化合物，或其药学上可接受的盐、酯或前药：具有抗菌特性。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受试者。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。
• 6,11-3c-bicyclic 8a-azalide derivatives
  申请人：Bartizal Kenneth F.

  公开号：US20090149398A1

  公开（公告）日：2009-06-11

  Compounds of Formula (I), and pharmaceutically acceptable salts, esters, and prodrugs thereof: (I) are disclosed, wherein A, B, D, L, X, Y, Z and R 2′ , are described herein. The compounds exhibit antibacterial properties. The compounds of Formula (I) can be employed to treat or prevent bacterial infections as compounds per se or in the form of pharmaceutically acceptable salts, esters, or prodrugs. The compounds and their salts, esters, and prodrugs can also be employed as ingredients in pharmaceutical compositions, optionally in combination with other antibacterial agents, for the treatment of bacterial infections. Processes for making the compounds are also disclosed.

  公式（I）的化合物，及其药学上可接受的盐、酯和前药：在此披露，其中A、B、D、L、X、Y、Z和R2'在此描述。这些化合物具有抗菌特性。公式（I）的化合物可用于治疗或预防细菌感染，作为化合物本身或作为药学上可接受的盐、酯或前药的形式。这些化合物及其盐、酯和前药还可作为药物组成中的成分，可选择地与其他抗菌剂组合，用于治疗细菌感染。还披露了制备这些化合物的方法。
• 8A,11-BICYCLIC 8A-AZALIDE DERIVATIVES
  申请人：Or Yat Sun

  公开号：US20070259822A1

  公开（公告）日：2007-11-08

  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.

  本发明揭示了化合物的结构式 I，或其药学上可接受的盐、酯或前药，具有抗菌特性。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受试者使用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。
• [EN] 9a, 11-3C-BICYCLIC 9a-AZALIDE DERIVATIVES<br/>[FR] DERIVES 9A-AZALIDE 11-3C-BICYCLIQUES
  申请人：ENANTA PHARM INC

  公开号：WO2005030227A1

  公开（公告）日：2005-04-07

  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.

  本发明公开了具有式(I)的化合物，或其药学上可接受的盐、酯或前药，这些化合物具有抗菌性能。本发明还涉及包括上述化合物的药物组合物，用于治疗需要抗生素治疗的受试者。该发明还涉及通过给受试者施用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。
• [EN] 3'-N-SUBSTITUTED-3-O-SUBSTITUTED ERYTHRONOLIDE A DERIVATIVES<br/>[FR] DERIVES D'ERYTHRONOLIDE A 3'-N-SUBSTITUES-3-O-SUBSTITUES
  申请人：RANBAXY LAB LTD

  公开号：WO2005030786A1

  公开（公告）日：2005-04-07

  This invention generally relates to macrolides, more particularly, the invention relates to 3-N-substituted-3-O-substituted erythronolide A derivatives, which are antibacterial agents effective against gram positive or gram negative bacteria and atypical pathogens. The compounds of this invention are more particularly effective against Staphylococcus aureus, Streptococcus pneumoniae, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa, Haemophilus influenzae. The invention also relates to a process for the preparation of the compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the methods for treating bacterial infection.

  本发明一般涉及大环内酯类化合物，更具体地，涉及3-N-取代-3-O-取代的红霉素A衍生物，它们是抗细菌药物，对革兰氏阳性或革兰氏阴性细菌和非典型病原体具有有效的作用。本发明的化合物对金黄色葡萄球菌、肺炎链球菌、肠球菌、大肠杆菌、铜绿假单胞菌、流感嗜血杆菌等尤其有效。本发明还涉及一种制备本发明化合物的方法，含有本发明化合物的制药组合物以及治疗细菌感染的方法。