8-amino-3-hydroxy-6H-benzo[c]chromen-6-one | 1026778-00-6

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 香豆素及其衍生物
• 英文名称: 8-amino-3-hydroxy-6H-benzo[c]chromen-6-one
• 英文别名: 8-Amino-3-hydroxybenzo[c]chromen-6-one
• CAS: 1026778-00-6
• 化学式: C₁₃H₉NO₃
• 分子量: 227.219
• InChiKey: MQEDFFUKYHEXTG-UHFFFAOYSA-N

物化性质

• 沸点：
  532.3±43.0 °C(Predicted)
• 密度：
  1.472±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  17
• 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：
  72.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  8-amino-3-hydroxy-6H-benzo[c]chromen-6-one 在 lithium aluminium tetrahydride 、 三丁基膦 、 碘 、 potassium carbonate 、 1,1'-azodicarbonyl-dipiperidine 作用下， 以 四氢呋喃 、 N-甲基吡咯烷酮 、 N,N-二甲基甲酰胺 、 苯 为溶剂， 反应 74.5h， 生成 5-(5-fluoro-2-methylphenoxymethyl)-6-(2-methoxy-4-methoxymethoxyphenyl)-2,2,4-trimethyl-1,2-dihydroquinoline
  参考文献：
  名称：

  GLUCOCORTICOID RECEPTOR AGONIST COMPOSED OF 2,2,4-TRIMETHYL-6-PHENYL-1,2-DIHYDROQUINOLINE DERIVATIVE HAVING SUBSTITUTED OXY GROUP

  摘要：

  公开号：

  EP2319835B1
• 作为产物：
  描述：

  3-hydroxy-8-nitro-6H-dibenzo[b,d]pyran-6-one 在 钯 氢气 、 甲醇 、 水 作用下， 以 甲醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 16.0h， 以to give the titled reference compound (44.02 g) as a pale yellow solid的产率得到8-amino-3-hydroxy-6H-benzo[c]chromen-6-one
  参考文献：
  名称：

  Glucocorticoid receptor agonist comprising 2,2,4-trimethyl-6-phenyl-1,2-dihydroquinoline derivatives having substituted oxy group

  摘要：

  本发明涉及一种由式（1）所表示的化合物组成的糖皮质激素受体激动剂或其盐，并且涉及所述糖皮质激素受体激动剂的新的药理作用。在式（1）中，R1表示式（2a）、（3a）、（4a）或（5a）；R2表示—（CO）—R8、—（CO）O—R9或类似物；R2—O—在苯环A的4-或5-位被取代；R3表示较低的烷基；R4、R5、R6或R7表示卤原子、可以有取代基的较低烷基或类似物；m、n、p或q表示0、1或类似物；R8、R9或类似物表示可以有取代基的较低烷基、较低烯基或类似物。

  公开号：

  US08426406B2

文献信息

• NOVEL 1,2-DIHYDROQUINOLINE DERIVATIVE HAVING (SUBSTITUTED PHENYL OR SUBSTITUTED HETEROCYCLIC) CARBONYLOXY LOWER ALKYL GROUP AND ESTER-INTRODUCED PHENYL GROUP AS SUBSTITUENTS
  申请人：Matsuda Mamoru

  公开号：US20090298826A1

  公开（公告）日：2009-12-03

  The compounds represented in general formula (1) and a salt thereof are useful for glucocorticoid receptor modulator. The R 1 represents a hydrogen atom or a lower alkyl group; R 2 represents a hydrogen atom or a lower alkyl group; R 3 and R 4 may be the same or different and represent a hydrogen atom or a lower alkyl group; R 5 represents a hydrogen atom or a lower alkyl group; R 6 represents a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, a nitro group or a cyano group; X represents —C(O)—, —C(O)NR 8 —, —S(O) 2 — and the like; R 7 and/or R 8 may be the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, a lower alkoxy group which may have a substituent and the like; Y represents a lower alkylene group; Z represents a benzene ring or a heterocyclic ring; and P represents 0, 1, 2 or 3.

  通用公式（1）中代表的化合物及其盐对糖皮质激素受体调节剂非常有用。其中，R1代表氢原子或较低的烷基基团；R2代表氢原子或较低的烷基基团；R3和R4可以相同也可以不同，代表氢原子或较低的烷基基团；R5代表氢原子或较低的烷基基团；R6代表卤素原子、较低的烷基基团、羟基、较低的烷氧基、硝基或氰基；X代表—C(O)—、—C(O)NR8—、—S(O)2—等；R7和/或R8可以相同也可以不同，代表氢原子、可能具有取代基团的较低烷基基团、可能具有取代基团的芳基、可能具有取代基团的杂环基团、可能具有取代基团的较低烷氧基团等；Y代表较低的烷基烯基团；Z代表苯环或杂环环；P代表0、1、2或3。
• NOVEL 1,2-DIHYDROQUINOLINE DERIVATIVE HAVING SUBSTITUTED PHENYLAMINO LOWER ALKYL GROUP AND ESTER-INTRODUCED PHENYL GROUP AS SUBSTITUENTS
  申请人：Matsuda Mamoru

  公开号：US20090298827A1

  公开（公告）日：2009-12-03

  The compounds represented in general formula (1) and a salt thereof are useful for glucocorticoid receptor modulator. The R 1 represents a hydrogen atom or a lower alkyl group; R 2 represents a hydrogen atom or a lower alkyl group; R 3 and R 4 may be the same or different and represents a hydrogen atom or a lower alkyl group; R 5 represents a hydrogen atom or a lower alkyl group; R 6 represents a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, a nitro group or a cyano group; X represents —C(O)—, —C(O)NR 8 —, —S(O) 2 — and the like; R 7 and/or R 8 may be the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, a lower alkoxy group which may have a substituent and the like; Y represents a lower alkylene group; and P represents 0, 1, 2 or 3.

  通式（1）及其盐对于糖皮质激素受体调节剂很有用。其中，R1代表氢原子或较低烷基；R2代表氢原子或较低烷基；R3和R4可以相同也可以不同，代表氢原子或较低烷基；R5代表氢原子或较低烷基；R6代表卤原子、较低烷基、羟基、较低烷氧基、硝基或氰基；X代表—C（O）—，—C（O）NR8—，—S（O）2—等；R7和/或R8可以相同也可以不同，代表氢原子、较低烷基（可能具有取代基）、芳基（可能具有取代基）、杂环基（可能具有取代基）、较低烷氧基（可能具有取代基）等；Y代表较低烷基烯基；P代表0、1、2或3。
• Method for preventing or treating a disease related to the glucocorticoid receptor
  申请人：Matsuda Mamoru

  公开号：US20110275620A1

  公开（公告）日：2011-11-10

  A method for preventing or treating a disease related to the glucocorticoid receptor involving administering a pharmacologically effective amount of a 1,2-hydroquinoline compound.

  一种预防或治疗与糖皮质激素受体相关的疾病的方法，涉及给予1,2-羟基喹啉化合物的药理有效剂量。
• 1,2-dihydroquinoline derivative having substituted phenylamino lower alkyl group and ester-introduced phenyl group as substituents
  申请人：Santen Pharmaceutical Co., Ltd.

  公开号：US08008498B2

  公开（公告）日：2011-08-30

  The compounds represented in general formula (1) and a salt thereof are useful for glucocorticoid receptor modulator. The R1 represents a hydrogen atom or a lower alkyl group; R2 represents a hydrogen atom or a lower alkyl group; R3 and R4 may be the same or different and represents a hydrogen atom or a lower alkyl group; R5 represents a hydrogen atom or a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, a nitro group or a cyano group; X represents —C(O)—, —C(O)NR8—, —S(O)2— and the like; R7 and/or R8 may be the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, a lower alkoxy group which may have a substituent and the like; Y represents a lower alkylene group; and P represents 0, 1, 2 or 3.

  通式（1）所代表的化合物及其盐对于糖皮质激素受体调节剂很有用。其中，R1代表氢原子或较低的烷基；R2代表氢原子或较低的烷基；R3和R4可以相同也可以不同，代表氢原子或较低的烷基；R5代表氢原子或较低的烷基；R6代表卤原子、较低的烷基、羟基、较低的烷氧基、硝基或氰基；X代表—C（O）—、—C（O）NR8—、—S（O）2—等；R7和/或R8可以相同也可以不同，代表氢原子、较低的烷基（可能有取代基）、芳基（可能有取代基）、杂环基（可能有取代基）、较低的烷氧基（可能有取代基）等；Y代表较低的烷基；P代表0、1、2或3。
• 1,2-dihydroquinoline derivative having (substituted phenyl or substituted heterocyclic) carbonyloxy lower alkyl group and ester-introduced phenyl group as substituents
  申请人：Santen Pharmaceutical Co., Ltd.

  公开号：US08008497B2

  公开（公告）日：2011-08-30

  The compounds represented in general formula (1) and a salt thereof are useful for glucocorticoid receptor modulator. The R1 represents a hydrogen atom or a lower alkyl group; R2 represents a hydrogen atom or a lower alkyl group; R3 and R4 may be the same or different and represent a hydrogen atom or a lower alkyl group; R5 represents a hydrogen atom or a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, a nitro group or a cyano group; X represents —C(O)—, —C(O)NR8—, —S(O)2— and the like; R7 and/or R8 may be the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, a lower alkoxy group which may have a substituent and the like; Y represents a lower alkylene group; Z represents a benzene ring or a heterocyclic ring; and P represents 0, 1, 2 or 3.

  通式（1）所代表的化合物及其盐对于糖皮质激素受体调节剂非常有用。其中，R1代表氢原子或较低的烷基；R2代表氢原子或较低的烷基；R3和R4可以相同也可以不同，代表氢原子或较低的烷基；R5代表氢原子或较低的烷基；R6代表卤原子、较低的烷基、羟基、较低的烷氧基、硝基或氰基；X代表-C（O）-、-C（O）NR8-、-S（O）2-等；R7和/或R8可以相同也可以不同，代表氢原子、较低的烷基（可能有取代基）、芳基（可能有取代基）、杂环基（可能有取代基）、较低的烷氧基（可能有取代基）等；Y代表较低的烷基；Z代表苯环或杂环环；P代表0、1、2或3。