1-ethyl-6-n-propyl-8-methylimidazo[1,5-d]-as-triazin-4(3H)-one | 84227-36-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 三嗪类
• 英文名称: 1-ethyl-6-n-propyl-8-methylimidazo[1,5-d]-as-triazin-4(3H)-one
• 英文别名: 1-Ethyl-8-methyl-6-propylimidazo[1,5-d][1,2,4]triazin-4(3H)-one；1-ethyl-8-methyl-6-propyl-3H-imidazo[1,5-d][1,2,4]triazin-4-one
• CAS: 84227-36-1
• 化学式: C₁₁H₁₆N₄O
• 分子量: 220.274
• InChiKey: ONHKIFLLHVZOSM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  59.3
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  1-(5-甲基-2-丙基-1H-咪唑-4-基)丙烷-1-酮 生成 1-ethyl-6-n-propyl-8-methylimidazo[1,5-d]-as-triazin-4(3H)-one
  参考文献：
  名称：

  Process for preparing

  摘要：

  本公开描述了一种新颖的制备1-(较低烷基)取代的6-n-丙基-8-烷基咪唑并三唑并[1,5-d]-嘧啶-4(3H)-酮衍生物的过程，这些衍生物可用作抗哮喘药物。

  公开号：

  US04395547A1

文献信息

• 1-Substituted-6-n-propyl-8-methylimidazo(1,5-d)-as-triazin-4(3H)-ones
  申请人：AMERICAN CYANAMID COMPANY

  公开号：EP0057289A1

  公开（公告）日：1982-08-11

  This disclosure describes new compounds and compositions of matter useful as anti-asthmatic agents and the method of meliorating asthma in mammals therewith, the novel active ingredients of said compositions of matter being certain 1-substituted-6-n-propyl-8-methylimidazo [1,5-d]-as-triazin-4(3H)-ones and/or the pharmacologically acceptable acid-addition salts thereof.

  本公开描述了可用作抗哮喘药的新化合物和物质组合物，以及用其改善哺乳动物哮喘的方法，所述物质组合物的新活性成分是某些 1-取代-6-正丙基-8-甲基咪唑并[1,5-d]-异三嗪-4(3H)-酮和/或其药理上可接受的酸加成盐。
• Process for preparing 1-substituted-6-n-propyl-8-methylimidazo(1,5-d)-as-triazin-4(3H)-ones
  申请人：AMERICAN CYANAMID COMPANY

  公开号：EP0085756A1

  公开（公告）日：1983-08-17

  This disclosure describes novel processes for the preparation of 2-(n-propyll-4-methyl-5-(lower alkanoyl) imidazoles which are useful as intermediates for the preparation of anti-asthmatic agents.

  本公开介绍了制备 2-(正丙基-4-甲基-5-(低级烷酰基)咪唑的新工艺，这些咪唑可用作制备抗哮喘药物的中间体。
• Imidazo[1,5-d][1,2,4]triazines as potential antiasthma agents
  作者：Rolf Paul、John A. Brockman、W. A. Hallett、John W. Hanifin、M. Ernestine Tarrant、Lawrence W. Torley、Francis M. Callahan、Paul F. Fabio、Bernard D. Johnson

  DOI：10.1021/jm00149a029

  日期：1985.11

  By using inhibition of histamine release from antigen-challenged, sensitized human basophils as a means of identifying a potentially prophylactic drug for the treatment of asthma, a series of substituted imidazo[1,5-d][1,2,4]triazines were found, which were active. These compounds were prepared by treating imidazolecarboxaldehydes with excess Grignard agent and then oxidizing the resulting alcohols to ketones with Jones reagent. Pyrolysis of a mixture of ketone and methyl carbazate at 200 degrees C in diphenyl ether produced the desired imidazo[1,5-d][1,2,4]triazines. Those compounds with the greatest basophil activity were tested for in vivo activity in the mouse passive cutaneous anaphylaxis (PCA) and the guinea pig passive anaphylaxis tests. The best compounds, 1-ethyl-8-methyl-6-propylimidazo[1,5-d][1,2,4]triazin-4(3H)- one (4-17) and 1,8-dimethyl-6-propylimidazo[1,5-d][1,2,4]triazin-4-(3H)-one (4-16) were chosen for further study.
• PAUL, R.;BROCKMAN, J. A.;HALLETT, W. A.;HANIFIN, J. W.;TARRANT, M. E.;TOR+, J. MED. CHEM., 1985, 28, N 11, 1704-1716
  作者：PAUL, R.、BROCKMAN, J. A.、HALLETT, W. A.、HANIFIN, J. W.、TARRANT, M. E.、TOR+

  DOI：——

  日期：——
• Verwendung von Aminoantipyrin-Verbindungen und neue Aminoantipyrinderivative
  申请人：BOEHRINGER MANNHEIM GMBH

  公开号：EP0033539B1

  公开（公告）日：1983-01-19