1H-Imidazol-2-amine, 1-(2,6-dichlorophenyl)-4-methyl- | 74680-56-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 1H-Imidazol-2-amine, 1-(2,6-dichlorophenyl)-4-methyl-
• 英文别名: 1-(2,6-dichlorophenyl)-4-methylimidazol-2-amine
• CAS: 74680-56-1
• 化学式: C₁₀H₉Cl₂N₃
• 分子量: 242.1
• InChiKey: BHFRZBBGQRDDKU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  43.8
• 氢给体数：
  1
• 氢受体数：
  2

文献信息

• 2,6-Dichlorophenyl-substituted amino-imidazole derivatives, processes of preparing such derivatives and pharmaceutical preparations comprising said derivatives
  申请人：Farmos-Yhtyma Oy

  公开号：EP0008150A2

  公开（公告）日：1980-02-20

  The 2,6-dichlorphenyl-substituted amino-imidazole derivatives 1-(2',6'-dichlorphenyl)-2-amino-4-methyl-imidazole, 2-(2',6'-dichloroanilino)-4-methyl-imidazole, their non-toxic, pharmaceutically acceptable, acid addition salts and mixtures thereof, exhibit excellent anti-hypertensive and anti-ulcer activities which makes the derivatives particularly suitable for treatment of high blood pressure and gastric ulcers in mammals. The derivatives may be prepared in either of two processes. The first process involves the sequential reaction of a known starting material with ammonia and a halogenated acetone which may be followed by separation of the formed isomers. The second process involves the decarboxylation of the novel intermediates 4-[1-(2',6'-dichlorphenyl)-2-amino)]-imidazoleacetic acid or 4-[2-(2',6'-dichloranilino)]-imidazoleacetic acid or mixtures thereof. The derivatives are employed in an effective amount and are typically combined with a pharmaceutical carrier. Administration of the derivatives may be accomplished either orally or parenterally.

  2,6-二氯苯基取代的氨基咪唑衍生物 1-(2',6'-二氯苯基)-2-氨基-4-甲基-咪唑、2-(2',6'-二氯苯胺基)-4-甲基-咪唑、它们的无毒、药学上可接受的酸加成盐及其混合物表现出卓越的抗高血压和抗溃疡活性，这使得这些衍生物特别适用于治疗哺乳动物的高血压和胃溃疡。 这些衍生物可以通过两种工艺中的任何一种来制备。第一种工艺是将已知的起始原料与氨和卤代丙酮进行连续反应，然后分离形成的异构体。第二个过程是新型中间体 4-[1-(2',6'-二氯苯基)-2-氨基)]-咪唑乙酸或 4-[2-(2',6'-二氯苯胺)]-咪唑乙酸或其混合物的脱羧反应。 这些衍生物以有效量使用，通常与药物载体结合。这些衍生物可以口服或肠外给药。
• US4275072A
  申请人：——

  公开号：US4275072A

  公开（公告）日：1981-06-23