2-Methoxy-5-(1-trityl-1H-imidazol-4-yl)-pyridine | 484673-50-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: 2-Methoxy-5-(1-trityl-1H-imidazol-4-yl)-pyridine
• 英文别名: 2-Methoxy-5-(1-tritylimidazol-4-yl)pyridine
• CAS: 484673-50-9
• 化学式: C₂₈H₂₃N₃O
• 分子量: 417.51
• InChiKey: CFXNCAINGOESLQ-UHFFFAOYSA-N

物化性质

• 沸点：
  579.4±50.0 °C(Predicted)
• 密度：
  1.12±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.7
• 重原子数：
  32
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  39.9
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-Methoxy-5-(1-trityl-1H-imidazol-4-yl)-pyridine 在 盐酸 、 potassium carbonate 作用下， 以 乙醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 36.0h， 生成 2-{4-[4-(6-methoxypyridin-3-yl)imidazol-1-yl]butyl}isoindole-1,3-dione
  参考文献：
  名称：

  Synthesis and Antibacterial Activity of Novel C₁₂ Vinyl Ketolides

  摘要：

  A novel series Of C-12 vinyl erythromycin derivatives have been discovered which exhibit in vitro and in vivo potency against key respiratory pathogens. The C-12 modification involves replacing the natural C-12 methyl group in the erythromycin core with a vinyl group via chemical synthesis. From the C-12 vinyl macrolide core, a series Of C-12 vinyl ketolides was prepared. Several compounds were found to be potent against macrolide-sensitive and -resistant bacteria. The C-12 vinyl ketolides 6j and 6k showed a similar antimicrobial spectrum and comparable activity to the commercial ketolide telithromycin. However, the pharmacokinetic profiles Of C-12 vinyl ketolides 6j and 6k in rats differ from that of telithromycin by having higher lung-to-plasma ratios, larger volumes of distribution, and longer half-lives. These pharmacokinetic differences have a pharmacodynamic effect as both 6j and 6k exhibited better in vivo efficacy than telithromycin in rat lung infection models against Streptococcus pneumoniae and Haemophilus influenzae.

  DOI：

  10.1021/jm051157a
• 作为产物：
  描述：

  5-溴-2-甲氧基吡啶 、 1-三苯甲基-4-碘咪唑 在 四(三苯基膦)钯 乙基溴化镁 、 zinc(II) chloride 作用下， 以 四氢呋喃 为溶剂， 反应 3.0h， 生成 2-Methoxy-5-(1-trityl-1H-imidazol-4-yl)-pyridine
  参考文献：
  名称：

  [EN] PYRIDYL SUBSTITUTED KETOLIDE ANTIBIOTICS
  [FR] ANTIBIOTIQUES A BASE DE KETOLIDE A SUBSTITUTION PYRIDYLE

  摘要：

  公开号：

  WO2004096822A3

文献信息

• C12 Modified erythromycin macrolides and ketolides having antibacterial activity
  申请人：——

  公开号：US20030125266A1

  公开（公告）日：2003-07-03

  Antimicrobial macrolide compounds are provided having formulas II: 1 as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

  提供具有II:1式的抗微生物大环内酯化合物，以及其药用盐、酯或前药；包含这类化合物的药物组合物；通过给予这类化合物治疗细菌感染的方法；以及这类化合物的制备方法。
• Pyridyl substituted ketolide antibiotics
  申请人：Burger T. Matthew

  公开号：US20050009764A1

  公开（公告）日：2005-01-13

  Antimicrobial macrolide and ketolide compounds are provided having formulas XII: as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

  提供具有XII式的抗微生物大环内酯和酮内酯化合物，以及其药学上可接受的盐、酯或前药；包含这些化合物的药物组合物；通过给予这些化合物的途径治疗细菌感染的方法；以及制备这些化合物的过程。
• [EN] NOVEL KETOLIDE DERIVATIVES<br/>[FR] NOUVEAUX DERIVES DE KETOLIDES
  申请人：CHIRON CORP

  公开号：WO2004096823A3

  公开（公告）日：2005-02-10
• C12 MODIFIED ERYTHROMYCIN MACROLIDES AND KETOLIDES HAVING ANTIBACTERIAL ACTIVITY
  申请人：CHIRON CORPORATION

  公开号：EP1404693A2

  公开（公告）日：2004-04-07
• US6756359B2
  申请人：——

  公开号：US6756359B2

  公开（公告）日：2004-06-29