1,2,3,4-tetrahydro-4-oxo-8-aminoquinoline | 50349-91-2

• 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: 1,2,3,4-tetrahydro-4-oxo-8-aminoquinoline
• 英文别名: 8-amino-2,3-dihydro-4(1H)-quinolinone；3-dihydro-8-amino-1H-quinolin-4-one；8-amino-2,3-dihydro-1H-quinolin-4-one；2,3-dihydro-8-amino-1H-quinolin-4-one；8-amino-2,3-dihydro-1H-quinolin-4-one；8-Amino-2,3-dihydro-1H-chinolin-4-on；4(1H)-Quinolinone, 8-amino-2,3-dihydro-
• CAS: 50349-91-2
• 化学式: C₉H₁₀N₂O
• 分子量: 162.191
• InChiKey: HQPFPBRBRITWKJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  55.1
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1,2,3,4-tetrahydro-4-oxo-8-aminoquinoline 在 盐酸 、 水 、 silica gel 作用下， 以 1,4-二氧六环 、 甲醇 、 水 为溶剂， 反应 35.0h， 生成 2-(2-hydroxycarbonyl-cyclopropyl)-4,5-dihydro-imidazo[4,5,1-ij]quinolin-6-one
  参考文献：
  名称：

  [EN] 4,5-DIHYDRO-IMIDAZO[4,5,1-J] QUINOLIN-6-ONES AS PARP INHIBITORS
  [FR] NOUVELLES 4,5-DIHYDRO-IMIDAZO[4,5,1-IJ]QUINOLIN-6-ONES

  摘要：

  公开号：

  WO2003103666A3
• 作为产物：
  描述：

  o-nitrobenzene 在 palladium 10% on activated carbon 氢氧化钾 、 氢气 、 phosphorus pentoxide 作用下， 以 甲醇 、 水 、 甲苯 为溶剂， 反应 19.5h， 生成 1,2,3,4-tetrahydro-4-oxo-8-aminoquinoline
  参考文献：
  名称：

  [EN] 4,5-DIHYDRO-IMIDAZO[4,5,1-II]QUINOLIN-6-ONES AS PARP INHIBITORS
  [FR] 4,5-DIHYDRO-IMIDAZO(4,5,1-IJ)QUINOLIN-6-ONES UTILISEES COMME INHIBITEURS DE PARP

  摘要：

  式1中，其中R1和R2具有描述中指示的含义的化合物是新颖的活性PARP抑制剂。

  公开号：

  WO2004108723A1

文献信息

• Imidazoquinoline derivatives
  申请人：Mochida Pharmaceutical Co., Ltd.

  公开号：US05856334A1

  公开（公告）日：1999-01-05

  Specified imidazoquinoline derivatives represented by the formula (I): ##STR1## where Q represents an optionally substituted phenyl, pyridyl or furyl group; Y represents either a hydrogen atom or, when taken together with Z, an oxygen atom and a methylene group; Z represents a hydrogen atom, a hydroxymethyl group, a carboxymethyl group, a 2-oxo-1-pyrrolidinyl group or the following formula (III): --A--R.sup.2 (III) (where A represents an oxygen atom, a sulfur atom or the group --NH--); or salts of such derivatives inhibit the increase of eosinophils and are useful as agents for preventing and/or treating diseases that manifest the increase of eosinophils.

  具有以下公式（I）所代表的特定咪唑喹啉衍生物：##STR1## 其中Q代表一个可选择取代的苯基、吡啶基或呋喃基；Y代表氢原子或者与Z一起取代时代表一个氧原子和一个亚甲基基团；Z代表氢原子、羟甲基基团、羧甲基基团、2-氧代-1-吡咯烷基基团或以下公式（III）：--A--R.sup.2 (III)（其中A代表一个氧原子、硫原子或基团--NH--）；或这些衍生物的盐，抑制嗜酸性粒细胞增加，并可用于预防和/或治疗表现为嗜酸性粒细胞增加的疾病。
• Tricyclic compound having anti-allergic activities
  申请人：Mochida Pharmaceutical Co., Ltd.

  公开号：US05643920A1

  公开（公告）日：1997-07-01

  A nitrogen-containing tricyclic compound represented by formula (I): ##STR1## a salt thereof, or a solvate of said compound or said salt, wherein R represents phenyl or naphthyl group which is unsubstituted or substituted at one to five sites with a group such as a halogen atom; a straight chain or branched alkyl group containing 1 to 10 carbon atoms which is unsubstituted or substituted with one or more halogen atoms; or the like; Y represents hydrogen atom; and Z represents a group such as hydrogen atom, hydroxyl group, or the like; or Y and Z together represent a group such as hydrazono group, hydroxyimino group, or the like which is unsubstituted or substituted with a particular group; and X.sup.1 -X.sup.2 .about.C.about.X.sup.3 represents CH--N--C.dbd.C or N--C.dbd.C--N; provided that when X.sup.1 -X.sup.2 .about.C.about.X.sup.3 represents N--C.dbd.C--N, Y and Z does not together represent hydroxyimino group or oxygen atom; is capable of inhibiting the production of IgE antibody, and therefore, is useful as a prophylactic and/or therapeutic agent for allergic diseases.

  一种含氮的三环化合物，由式(I)所代表：##STR1## 其盐，或者该化合物或盐的溶剂化合物，其中R代表未取代或在一个到五个位置取代的苯基或萘基，取代基可以是卤原子等；一种含有1到10个碳原子的直链或支链烷基基团，未取代或取代有一个或多个卤原子；或类似物；Y代表氢原子；Z代表氢原子、羟基基团等基团；或者Y和Z一起代表未取代或取代有特定基团的肼酮基团、羟亚胺基团等基团；X.sup.1 -X.sup.2 .about.C.about.X.sup.3代表CH--N--C.dbd.C或N--C.dbd.C--N；但当X.sup.1 -X.sup.2 .about.C.about.X.sup.3代表N--C.dbd.C--N时，Y和Z不应一起代表羟亚胺基团或氧原子；能够抑制IgE抗体的产生，因此，可用作过敏疾病的预防和/或治疗药物。
• Mild and Safer Preparative Method for Nonsymmetrical Sulfamides via <i>N</i>-Sulfamoyloxazolidinone Derivatives:  Electronic Effects Affect the Transsulfamoylation Reactivity
  作者：A. Borghese、L. Antoine、J. P. Van Hoeck、Mockel、A. Merschaert

  DOI：10.1021/op0600106

  日期：2006.7.1

  phosphorus oxychloride, or phosphorus pentachloride. We report here a safer and more convenient synthetic methodology for large-scale preparation of sulfamides using the N-substituted oxazolidin-2-one derivatives 5 as synthetic equivalent of the corrosive and hazardous N-sulfamoyl chloride. The scope of the use of N-sulfamoyloxazolidinones to prepare nonsymmetrical sulfamides is explored.

  磺酰胺（R 1 R 2 N-SO 2 -NR 3 R 4）通常是使用强亲电试剂和有害试剂（例如N-氨磺酰氯，磺酰氯，三氯氧化磷或五氯化磷）制备的。我们在此报告了一种更安全，更方便的合成方法，该方法可使用N-取代的恶唑烷-2-酮衍生物5作为腐蚀性和有害的N-氨磺酰氯的合成等效物，大规模制备磺酰胺。探索了使用N-氨磺酰基恶唑烷酮制备非对称磺酰胺的范围。
• 4,5-dihydro-6H-imidazo[4,5,1-ij]quinolin-6-one-6-oxime-O-sulfonic acid
  申请人：Mochida Pharmaceutical Co., Ltd.

  公开号：US05151431A1

  公开（公告）日：1992-09-29

  The present invention relates to novel 4,5-dihydro-6H-imidazo[4,5,1-ij]quinolin-6-one-6-oxime-O-sulfonic acid compounds, processes for producing said compounds, intermediate compounds, i.e. novel 4,5-dihydro-6H-imidazo[4,5,1-ij]quinolin-6-one compounds and 4,5-dihydro-6H-imidazo[4,5,1-ij]quinolin-6-one-6-oxime compounds in the synthesis of said compounds, processes for producing said intermediate compounds, and pharmaceutical or veterinary compositions containing said compounds. The present invention is based on the selection of the substituents of 4,5-dihydro-6H-imidazo[4,5,1-ij]-quinolin-6-one-6-oxime-O-sulfonic acid compounds at 2-position, namely 2-(2-penten-3-yl)-, 2-cyclohexyl-, 2-naphthyl-, 2-thienyl-, etc. The compounds of the present invention containing these substituents have potent hypotensive, anti-oedematous and diuretic effects as well as an activity of removing ascites. The compounds of the present invention are extremely useful for treatment of diseases and disorders mentioned above.

  本发明涉及新的4,5-二氢-6H-咪唑并[4,5,1-ij]喹啉-6-酮-6-肟-O-磺酸化合物，制备该化合物的方法，中间体化合物，即新的4,5-二氢-6H-咪唑并[4,5,1-ij]喹啉-6-酮化合物和4,5-二氢-6H-咪唑并[4,5,1-ij]喹啉-6-酮-6-肟化合物在该化合物的合成中的应用，制备该中间体化合物的方法，以及含有该化合物的药物或兽医组合物。本发明基于在2位处选择4,5-二氢-6H-咪唑并[4,5,1-ij]-喹啉-6-酮-6-肟-O-磺酸化合物的取代基，即2-(2-戊烯-3-基)-、2-环己基-、2-萘基-、2-噻吩基-等。本发明的含有这些取代基的化合物具有强效的降压、抗水肿和利尿作用，以及除去腹水的活性。本发明的化合物对于上述疾病和障碍的治疗非常有用。
• 4,5-Dihydro-6H-imidazo[4,5,1-ij]quinolin-6-one-6-oxime-O-sulfonic acid derivatives
  申请人：MOCHIDA PHARMACEUTICAL CO., LTD.

  公开号：EP0405442A1

  公开（公告）日：1991-01-02

  The present invention relates to novel 4,5-dihydro-6H-imidazo[4,5,1-ij]quinolin-6-one-6-oxime-0-sulfonic acid compounds, processes for producing said compounds, intermediate compounds, i.e. novel 4,5-dihydro-6H-imidazo[4,5,1-ij]quinolin-6-one compounds and 4,5-dihydro-6H-imidazo[4,5,1-ij]quinolin-6-one-6-oxime compounds in the synthesis of said compounds, processes for producing said intermediate compounds, and pharmaceutical or veterinary compositions containing said compounds. The present invention is based on the selection of the substituents of 4,5-dihydro-6H-imidazo[4,5,1-ij]-quinolin-6-one-6-oxime-O-sulfonic acid compounds at 2-position, namely 2-(2-penten-3-yl)-, 2-cyclohexyl-, 2-naphthyl-, 2-thienyl-, etc. The compounds of the present invention containing these substituents have potent- hypotensive, antioedematous and diuretic effects as well as an activity of removing ascites. The compounds of the present invention are extremely useful for treatment of diseases and disorders mentioned above.

  本发明涉及新型 4,5-二氢-6H-咪唑并[4,5,1-ij]喹啉-6-酮-6-肟-0-磺酸化合物、生产上述化合物的工艺、中间化合物，即新型 4,5-二氢-6H-咪唑并[4,5,1-ij]喹啉-6-酮化合物和合成所述化合物的 4,5-二氢-6H-咪唑并[4,5,1-ij]喹啉-6-酮-6-肟化合物，生产所述中间化合物的工艺，以及含有所述化合物的药物或兽药组合物。 本发明基于对 4,5-二氢-6H-咪唑并[4,5,1-ij]-喹啉-6-酮-6-肟-O-磺酸化合物 2-位取代基的选择，即 2-(2-戊烯-3-基)-、2-环己基-、2-萘基-、2-噻吩基-等。 含有这些取代基的本发明化合物具有强效降血压、消肿和利尿作用，并具有去除腹水的活性。本发明的化合物对治疗上述疾病和失调非常有用。