(4-甲基-6-吗啉-4-基哒嗪-3-基)肼 | 37121-78-1

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: (4-甲基-6-吗啉-4-基哒嗪-3-基)肼
• 英文名称: (4-Methyl-6-morpholin-4-yl-pyridazin-3-yl)-hydrazine
• 英文别名: Morpholine, 4-(6-hydrazino-5-methyl-2-pyridazinyl)-, dihydrochloride, hydrate；(4-methyl-6-morpholin-4-ylpyridazin-3-yl)hydrazine
• CAS: 37121-78-1
• 化学式: C₉H₁₅N₅O
• 分子量: 209.251
• InChiKey: GQMWSPOOCHFOKY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  76.3
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  (4-甲基-6-吗啉-4-基哒嗪-3-基)肼 、 甲酸 在 氯仿 、 Sodium sulfate-III 作用下， 以to obtain the 8-methyl-6-morpholino-s-triazolo[4,3-b]pyridazine product as the free base的产率得到8-methyl-6-morpholino[1,2,4]triazolo[4,3-b]pyridazine
  参考文献：
  名称：

  Triazolopyridazines used to alleviate bronchial spasms

  摘要：

  本发明涉及一种方法，通过向哺乳动物施用3,6,8-取代的三唑并吡嗪化合物，如8-甲基-6-吗啡基-s-三唑并[4,3-b]吡嗪、3,8-二甲基-6-哌啶基-s-三唑并[4,3-b]吡嗪或其药学上可接受的盐，用于对抗哺乳动物的支气管痉挛。

  公开号：

  US04136182A1

文献信息

• 6-Morpholino-3-substituted phenyl-S-triazolo[4,3-b]pyridazines
  申请人：Gruppo Lepetit S.p.A.

  公开号：US04016162A1

  公开（公告）日：1977-04-05

  6-Morpholino-3-substituted phenyl triazolopyridazine compounds such as 8-methyl-6-morpholino-3-phenyl-s-triazolo[4,3-b]pyridazine or 8-methyl-6-morpholino-3-(3,4,5-trimethoxyphenyl)-s-triazolo[4,3-b]pyridazi ne are prepared by the reaction of the corresponding substituted benzoyl halide with a 3-hydrazino-6-morpholinopyridazine in the presence of a hydrogen chloride acceptor or by the reaction of a 3-halo-6-morpholinopyridazine with a corresponding substituted benzoyl hydrazide. The compounds have pharmacological activity as bronchodilators.

  6-吗啡啉基-3-取代苯基三唑并吡啶类化合物，如8-甲基-6-吗啡啉基-3-苯基-s-三唑并[4,3-b]吡啶或8-甲基-6-吗啡啉基-3-(3,4,5-三甲氧基苯基)-s-三唑并[4,3-b]吡啶，通过相应取代苯甲酰卤与3-吗啡啉基-6-吗啡啉基吡啶在氢氯酸受体存在下反应制备，或通过3-卤代-6-吗啡啉基吡啶与相应取代苯甲酰肼反应制备。这些化合物具有支气管扩张剂的药理活性。
• Antihypertensives. N-1H-Pyrrol-1-yl-3-pyridazinamines
  作者：Elvio Bellasio、Ambrogio Campi、Nunzio Di Mola、Emiliana Baldoli

  DOI：10.1021/jm00374a024

  日期：1984.8

  The hypothesis that the side effects of hydralazine, such as mutagenicity and lupus erythematosus like syndrome, might be due to the NHNH2 group prompted us to incorporate part of this moiety into a pyrrole ring. Therefore, we prepared a series of N-1H-pyrrol-1-yl-3-pyridazinamines and a limited number of N-1H-pyrrol-1-yl-1-phthalazinamines by reaction of 3-hydrazinopyridazines and 1-hydrazinophthalazines with gamma-diketones. Most of these compounds, especially in the pyridazine series, showed moderate to strong antihypertensive activity in spontaneously hypertensive rats. The decrease in blood pressure generally had a slow onset after either oral or intravenous administration. N-(2,5-Dimethyl-1H-pyrrol-1-yl)-6-(4-morpholinyl)-3-pyridazinamine hydrochloride (30) (MDL 899) showed no mutagenic activity in several tests and is now in clinical trials in patients.
• US4016162A
  申请人：——

  公开号：US4016162A

  公开（公告）日：1977-04-05
• US4136182A
  申请人：——

  公开号：US4136182A

  公开（公告）日：1979-01-23
• Triazolopyridazines used to alleviate bronchial spasms
  申请人：The Dow Chemical Company

  公开号：US04136182A1

  公开（公告）日：1979-01-23

  This invention relates to a method useful for combatting bronchial spasm in mammals by means of administering to mammals a 3,6,8-substituted triazolopyridazine compound such as 8-methyl-6-morpholino-s-triazolo-[4,3-b]pyridazine, 3,8-dimethyl-6-piperidino-s-triazolo-[4,3-b]pyridazine or a pharmacologically-acceptable salt thereof.

  本发明涉及一种方法，通过向哺乳动物施用3,6,8-取代的三唑并吡嗪化合物，如8-甲基-6-吗啡基-s-三唑并[4,3-b]吡嗪、3,8-二甲基-6-哌啶基-s-三唑并[4,3-b]吡嗪或其药学上可接受的盐，用于对抗哺乳动物的支气管痉挛。