2-(2-tert-butyldimethylsiloxyethyl)-3,4-dihydro-6-methoxy-3-oxo-2H-1,4-benzoxazine | 191097-23-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并恶嗪类
• 英文名称: 2-(2-tert-butyldimethylsiloxyethyl)-3,4-dihydro-6-methoxy-3-oxo-2H-1,4-benzoxazine
• 英文别名: 2-{[tert-Butyl(dimethyl)silyl]oxy}ethyl-6-methoxy-2H-1,4-benzoxazin-3(4H)-one；2-[2-[tert-butyl(dimethyl)silyl]oxyethyl]-6-methoxy-4H-1,4-benzoxazin-3-one
• CAS: 191097-23-1
• 化学式: C₁₇H₂₇NO₄Si
• 分子量: 337.491
• InChiKey: DNZPFEOBIVABGB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.81
• 重原子数：
  23
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.59
• 拓扑面积：
  56.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-(2-tert-butyldimethylsiloxyethyl)-3,4-dihydro-6-methoxy-3-oxo-2H-1,4-benzoxazine 生成 4-(3-Chlorobenzyl)-3,4-dihydro-2-(2-hydroxyethyl)-3-oxo-6-methoxy 2H-1,4-benzoxazine
  参考文献：
  名称：

  Benzoxazine antimicrobial agents

  摘要：

  该发明涉及一般式为：##STR1##的苯并噁嗪和吡啶噁嗪抗菌化合物，其中基团Q是如本文所述的融合苯或融合吡啶基团，含有这些化合物的药物组合物，其生产方法以及在治疗细菌感染中的应用。

  公开号：

  US05696117A1
• 作为产物：
  描述：

  4-甲氧基-2-硝基酚 在 palladium on activated charcoal 咪唑 、 氢气 、 potassium carbonate 作用下， 以 乙醇 、 N,N-二甲基甲酰胺 为溶剂， 生成 2-(2-tert-butyldimethylsiloxyethyl)-3,4-dihydro-6-methoxy-3-oxo-2H-1,4-benzoxazine
  参考文献：
  名称：

  Benzoxazinones as PPARγ agonists. part 1: SAR of three aromatic regions

  摘要：

  A series of benzoxazinones was synthesized as PPARgamma agonists. The compounds were obtained in seven steps, and SAR was developed by variations to the core shown below. The compounds were tested as functional agonists in the induction of the aP2 gene in preadipocytes, and the most potent compound in the series has an EC50=0.51 muM. The potency was further confirmed through a PPAR-Ga14 construct. Efficacy has been demonstrated in the db/db mouse model of hyperglycemia. (C) 2003 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(03)00401-3

文献信息

• Compounds for the treatment of multi-drug resistant bacterial infections
  申请人：AstraZeneca AB

  公开号：US07875715B2

  公开（公告）日：2011-01-25

  The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans.

  本发明涉及表现出抗菌活性的化合物，其制备过程，含有其作为活性成分的药物组合物，以及它们作为药物的使用和用于制造用于治疗温血动物（如人类）细菌感染的药物的使用。特别地，本发明涉及用于治疗温血动物（如人类）细菌感染的有用化合物，更具体地涉及这些化合物用于制造用于治疗温血动物（如人类）细菌感染的药物。
• Benzoxazine antimicrobial agents
  申请人：Ortho Pharmaceutical Corporation

  公开号：US05696117A1

  公开（公告）日：1997-12-09

  The invention relates to benzoxazine and pyrido-oxazine antibacterial compounds of the general formula: ##STR1## wherein the moiety Q is a fused phenyl or fused pyridyl moiety as herein described, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.

  该发明涉及一般式为：##STR1##的苯并噁嗪和吡啶噁嗪抗菌化合物，其中基团Q是如本文所述的融合苯或融合吡啶基团，含有这些化合物的药物组合物，其生产方法以及在治疗细菌感染中的应用。
• Benzoxazinones as PPARγ agonists. part 1: SAR of three aromatic regions
  作者：Philip J. Rybczynski、Roxanne E. Zeck、Donald W. Combs、Ignatius Turchi、Thomas P. Burris、Jun Z. Xu、Maria Yang、Keith T. Demarest

  DOI：10.1016/s0960-894x(03)00401-3

  日期：2003.7

  A series of benzoxazinones was synthesized as PPARgamma agonists. The compounds were obtained in seven steps, and SAR was developed by variations to the core shown below. The compounds were tested as functional agonists in the induction of the aP2 gene in preadipocytes, and the most potent compound in the series has an EC50=0.51 muM. The potency was further confirmed through a PPAR-Ga14 construct. Efficacy has been demonstrated in the db/db mouse model of hyperglycemia. (C) 2003 Elsevier Science Ltd. All rights reserved.