1,4-dihydro-1,N-dimethyl-4-oxo-3-quinolinesulfonamide | 49667-11-0

• 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: 1,4-dihydro-1,N-dimethyl-4-oxo-3-quinolinesulfonamide
• 英文别名: 1-methyl-4-oxo-1,4-dihydro-quinoline-3-sulfonic acid methylamide；1,N-dimethyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide；N,1-dimethyl-4-oxoquinoline-3-sulfonamide
• CAS: 49667-11-0
• 化学式: C₁₁H₁₂N₂O₃S
• 分子量: 252.294
• InChiKey: UMBKNZYONDDZAF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  74.9
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  4-甲基氨基-N-甲基-3-喹啉磺酰胺 在 sodium hydroxide 作用下， 以 水 为溶剂， 反应 1.5h， 生成 1,4-dihydro-1,N-dimethyl-4-oxo-3-quinolinesulfonamide
  参考文献：
  名称：

  The Preparation of 1-Methyl- (and Ethyl)-1,4-dihydro-4-oxo- and 4-thioxo-3-quinolinesulfonamides from 4-Amino-3-quinolinesulfonamides

  摘要：

  DOI：

  10.3987/com-99-8607

文献信息

• Quinolone sulphonamides useful as antihypertensive agents
  申请人：The Boots Company

  公开号：US04772614A1

  公开（公告）日：1988-09-20

  Quinolones with antihypertensive activity have the general formula I, ##STR1## wherein X is the residue of an optionally substituted benzene ring; R is lower alkyl; R.sub.3 is hydrogen or lower alkyl; R.sub.1 and R.sub.2, which may be the same or different, are hydrogen, lower alkyl, or, together with the nitrogen atom to which they are attached, form a 5 to 7 membered saturated heterocyclic ring optionally containing an additional hetero atom selected from nitrogen, oxygen and sulphur and optionally substituted by 1 or more lower alkyl groups; and the dotted line between positions 2 and 3 of the quinolone nucleus represents an optional bond. The compounds are useful as antihypertensive agents. They are also indicated for use in treating heart failure and ischaemic heart disease. With the exception of the three compounds 1-methyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide, 1,N-dimethyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide and 6,7-dimethoxyl-methyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide, the quinolones of formula I are novel. Pharmaceutical compositions containing the compounds of formula I are described. Processes for preparing the novel quinolones are also described.

  具有降压活性的喹诺酮具有一般式I，其中X是可选择取代的苯环的残基；R是低碳烷基；R.sub.3是氢或低碳烷基；R.sub.1和R.sub.2，可以相同也可以不同，是氢、低碳烷基，或者与它们连接的氮原子一起形成一个含有氮、氧和硫的额外杂原子的5到7元饱和杂环环，可选择地由1个或多个低碳烷基取代；喹诺酮核的2和3位置之间的虚线代表一个可选键。这些化合物可用作降压剂。它们还适用于治疗心力衰竭和缺血性心脏病。除了三种化合物1-甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺、1,N-二甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺和6,7-二甲氧基甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺之外，一般式I的喹诺酮是新颖的。描述了含有一般式I化合物的制药组合物。还描述了制备新型喹诺酮的方法。
• Quinolones having antihypertensive activity
  申请人：The Boots Company PLC

  公开号：EP0206616A2

  公开（公告）日：1986-12-30

  Quinolines with antihypertensive activity have the general formula 1, wherein X is the residue of an optionally substituted benzene ring; R is lower alkyl; R3 is hydrogen or lower alkyl; R1 and R2, which may be the same or different, are hydrogen, lower alkyl, or, together with the nitrogen atom to which they are attached, form a 5 to 7 membered saturated heterocyclic ring optionally containing an additional hetero atom selected from nitrogen, oxygen and sulphur and optionally substituted by 1 or more lower alkyl groups; and the dotted line between positions 2 and 3 of the quinolone nucleus represents an optional bond. The compounds are useful as antihypertensive agents. They are also indicated for use in treating heart failure and ischaemic heart disease. With the exception of the three compounds 1-methyl-4--oxo-1,4-dihydroquinoline-3-sulphonamide, 1,N-dimethyl-4--oxo-1,4-dihydroquinoline-3-sulphonamide and 6,7-dimeth- oxyl-methyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide, the quinolones of formula I are novel. Pharmaceutical compositions containing the compounds of formula I are described. Processes for preparing the novel quinolones are also described.

  具有抗高血压活性的喹啉类化合物具有通式 1、 其中，X 是任选取代的苯环的残基；R 是低级烷基；R3 是氢或低级烷基；R1 和 R2（可以相同或不同）是氢、低级烷基，或与它们连接的氮原子一起形成 5 至 7 个成员的饱和杂环，其中任选含有一个选自氮、氧和硫的杂原子，并任选被 1 个或多个低级烷基取代；喹诺酮核的位置 2 和 3 之间的虚线代表任选键。这些化合物可用作降压药。它们还可用于治疗心力衰竭和缺血性心脏病。 除了 1-甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺、1,N-二甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺和 6,7-二甲基-氧代-4-甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺这三种化合物外，式 I 中的喹诺酮类化合物均为新型化合物。 描述了含有式 I 化合物的药物组合物。还描述了制备新型喹诺酮类药物的工艺。
• Therapeutic agents
  申请人：——

  公开号：EP0206616A3

  公开（公告）日：1988-06-01

  Quinolines with antihypertensive activity have the general formula 1, wherein X is the residue of an optionally substituted benzene ring; R is lower alkyl; R3 is hydrogen or lower alkyl; R1 and R2, which may be the same or different, are hydrogen, lower alkyl, or, together with the nitrogen atom to which they are attached, form a 5 to 7 membered saturated heterocyclic ring optionally containing an additional hetero atom selected from nitrogen, oxygen and sulphur and optionally substituted by 1 or more lower alkyl groups; and the dotted line between positions 2 and 3 of the quinolone nucleus represents an optional bond. The compounds are useful as antihypertensive agents. They are also indicated for use in treating heart failure and ischaemic heart disease.With the exception of the three compounds 1-methyl-4--oxo-1,4-dihydroquinoline-3-sulphonamide, 1,N-dimethyl-4--oxo-1,4-dihydroquinoline-3-sulphonamide and 6,7-dimeth- oxyl-methyl-4-oxo-1,4-dihydroquinoline-3-sulphonamide, the quinolones of formula I are novel.Pharmaceutical compositions containing the compounds of formula I are described. Processes for preparing the novel quinolones are also described.

  具有抗高血压活性的喹啉类化合物具有通式 1、 其中，X 是任选取代的苯环的残基；R 是低级烷基；R3 是氢或低级烷基；R1 和 R2（可以相同或不同）是氢、低级烷基，或与它们连接的氮原子一起形成 5 至 7 个成员的饱和杂环，其中任选含有一个选自氮、氧和硫的杂原子，并任选被 1 个或多个低级烷基取代；喹诺酮核的位置 2 和 3 之间的虚线代表任选键。这些化合物可用作降压药。除了 1-甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺、1,N-二甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺和 6,7-二甲基-氧代-甲基-4-氧代-1,4-二氢喹啉-3-磺酰胺这三种化合物外，式 I 的喹诺酮类化合物均为新型化合物。还描述了制备新型喹诺酮类药物的工艺。
• The Preparation of 1-Nonsubstituted and 1-Methyl- (and Ethyl)-1,4-dihydro-4-oxo- 3-quinolinesulfonamides from 4-Chloro-3-quinolinesulfonamides
  作者：Andrzej Maslankiewicz、Leszek Skrzypek

  DOI：10.3987/com-97-7887

  日期：——
• US4772614A
  申请人：——

  公开号：US4772614A

  公开（公告）日：1988-09-20