oxazolo[4,5-c]quinolin-4(5H)-one | 64220-10-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: oxazolo[4,5-c]quinolin-4(5H)-one
• 英文别名: Oxazolo<4,5-c>chinolin-4(5H)-on；5H-oxazolo[4,5-c]quinolin-4-one；5H-[1,3]oxazolo[4,5-c]quinolin-4-one
• CAS: 64220-10-6
• 化学式: C₁₀H₆N₂O₂
• 分子量: 186.17
• InChiKey: CZZJTLFINCRIQK-UHFFFAOYSA-N

物化性质

• 熔点：
  >270 °C(Solv: dimethyl sulfoxide (67-68-5))
• 沸点：
  275.5±9.0 °C(Predicted)
• 密度：
  1.382±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  14
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  55.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  oxazolo[4,5-c]quinolin-4(5H)-one 以7%的产率得到
  参考文献：
  名称：

  SUZUKI M.; MATSUMOTO K.; MIYOSHI M.; YONEDA N.; ISHIDA R., CHEM. AND PHARM. BULL. , 1977, 25, NO 10, 2602-2607

  摘要：

  DOI：
• 作为产物：
  描述：

  1H-3-amino-2-oxo-4-hydroxyquinoline 、 原甲酸三乙酯 反应 5.0h， 以93%的产率得到oxazolo[4,5-c]quinolin-4(5H)-one
  参考文献：
  名称：

  4-Hydroxy-2-quinolones. 36. Synthesis of 2-R-oxazolo[4,5-c]quinolin-4(5H)-ones

  摘要：

  DOI：

  10.1007/bf02320336

文献信息

• A synthesis of 3-amino-4-hydroxyquinolin-2(1H)-one derivatives via oxazolo[4,5-c]quinolin-4(5H)-ones.
  作者：MAMORU SUZUKI、KAZUO MATSUMOTO、MUNEJI MIYOSHI、NAOTO YONEDA、RYUICHI ISHIDA

  DOI：10.1248/cpb.25.2602

  日期：——

  3-Amino-4-hydroxyquinolin-2 (1H)-one compounds (aminocarbostyrils) were synthesized by a reaction of methyl isocyanoacetate with isatoic anhydrides in the presence of 1, 8-diazabicyclo [5, 4, 0] undec-7-ene (DBU), followed by hydrolysis with HCl. The alkylation of oxazolo [4, 5-c] quinolin-4 (5H)-ones which are the intermediates of the aminocarbostyrils and the acylation of aminocarbostyrils were also investigated. Furthermore, a variety of the quinolin-2 (1H)-one analogs showed antiallergic activity.

  在 1, 8-二氮杂双环 [5, 4, 0] 十一-7-烯 (DBU) 存在下，通过异氰基乙酸甲酯与异酸酐反应，然后用盐酸水解，合成了 3-氨基-4-羟基喹啉-2 (1H) -酮化合物（氨基卡波胆碱）。此外，还研究了恶唑并 [4, 5-c] 喹啉-4 (5H)- 酮（氨基卡波胆碱的中间体）的烷基化以及氨基卡波胆碱的酰化。此外，多种喹啉-2 (1H)-酮类似物显示出抗过敏活性。
• ZWITTERIONIC BICYCLIC COMPOUNDS AND THEIR SALTS, SOLVATES, HYDRATES AND ESTERS
  申请人：SCHERING CORPORATION

  公开号：EP0232328B1

  公开（公告）日：1992-04-15
• [EN] ANTIBACTERIAL COMPOUNDS<br/>[FR] COMPOSÉS ANTIBACTÉRIENS
  申请人：REDX PHARMA PLC

  公开号：WO2016024096A1

  公开（公告）日：2016-02-18

  This invention relates to antibacterial drug compounds containing a tricyclic ring system. It also relates to pharmaceutical formulations of antibacterial drug compounds. It also relates to uses of the derivatives in treating bacterial infections and in methods of treating bacterial infections. The invention is also directed to antibacterial drug compounds which are capable of treating bacterial infections which are currently hard to treat with existing drug compounds.