3-(piperidinocarbonylamino)pyridazine | 71344-26-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 3-(piperidinocarbonylamino)pyridazine
• 英文别名: piperidine-1-carboxylic acid pyridazin-3-ylamide；N-pyridazin-3-ylpiperidine-1-carboxamide
• CAS: 71344-26-8
• 化学式: C₁₀H₁₄N₄O
• 分子量: 206.247
• InChiKey: JSMYVONWCJRZCO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  58.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  哌啶 、 [1,2,4]oxadiazolo[2,3-b]pyridazine-2-thione 以 二甲基亚砜 为溶剂， 反应 2.0h， 以59%的产率得到3-(piperidinocarbonylamino)pyridazine
  参考文献：
  名称：

  Thermal decomposition of 2H-(1,2,4)oxadiazolo(2,3-a)pyridine-2-thione and 2H-(1,2,4)oxadiazolo(2,3-b)pyridazine-2-thiones: Generation of aza-heteroaromatic .ALPHA.-isocyanates and their utilization for the synthesis of unsymmetrical disubstituted ureas.

  摘要：

  2H-[1, 2, 4]噁二唑[2, 3-a]吡啶-2-硫酮的热分解生成了3-(2-吡啶基)-2H-吡啶[1, 2-a]-1, 3, 5-三嗪-2, 4(3H)-二酮和1, 3-二(2-吡啶基)脲，而其吡唑类似物的类似分解则生成了3-(3-吡唑基)-2H-吡唑[1, 6-a]-1, 3, 5-三嗪-2, 4(3H)-二酮和1, 3-二(3-吡唑基)脲。在分解过程中产生的氮杂杂环α-异氰酸酯被用于合成不对称的1, 3-二取代脲。

  DOI：

  10.1248/cpb.28.3570

文献信息

• ETHER BENZYLIDENE PIPERIDINE ARYL CARBOXAMIDE COMPOUNDS USEFUL AS FAAH INHIBITORS
  申请人：Fay Lorraine Kathleen

  公开号：US20110144159A1

  公开（公告）日：2011-06-16

  The present invention relates to compounds of Formula (I) wherein Ar is optionally substituted phenyl or 6-membered heteroaryl moiety, or a benzisoxazole, pyrrolopyridine, or benzotriazole group; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, including pain, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease.

  本发明涉及式(I)的化合物，其中Ar是可选的取代苯基或6元杂环基团，或苯并异噁唑、吡咯吡啶或苯并三氮唑基团；或其药学上可接受的盐；制备该化合物的过程；制备该化合物的中间体；含有该化合物的组合物；以及在治疗与脂肪酸酰胺水解酶（FAAH）活性相关的疾病或病症中使用该化合物，包括疼痛、尿失禁、过度活动的膀胱、呕吐、认知障碍、焦虑、抑郁、睡眠障碍、进食障碍、运动障碍、青光眼、牛皮癣、多发性硬化症、脑血管疾病、脑损伤、胃肠疾病、高血压或心血管疾病。
• OHSAWA A.; ARAI H.; IGETA H., HETEROCYCLES, 1979, 12, NO 7, 917-920
  作者：OHSAWA A.、 ARAI H.、 IGETA H.

  DOI：——

  日期：——
• OHSAWA AKIO; ARAI HEIHACHIRO; IGETA HIROSHI, CHEM. AND PHARM. BULL., 1980, 28, NO 12, 3570-3575
  作者：OHSAWA AKIO、 ARAI HEIHACHIRO、 IGETA HIROSHI

  DOI：——

  日期：——
• Thermal decomposition of 2H-(1,2,4)oxadiazolo(2,3-a)pyridine-2-thione and 2H-(1,2,4)oxadiazolo(2,3-b)pyridazine-2-thiones: Generation of aza-heteroaromatic .ALPHA.-isocyanates and their utilization for the synthesis of unsymmetrical disubstituted ureas.
  作者：AKIO OHSAWA、HEIHACHIRO ARAI、HIROSHI IGETA

  DOI：10.1248/cpb.28.3570

  日期：——

  Thermal decomposition of 2H-[1, 2, 4] oxadiazolo [2, 3-a] pyridine-2-thione afforded 3-(2-pyridyl)-2H-pyrido [1, 2-a]-1, 3, 5-triazine-2, 4 (3H)-dione and 1, 3-di (2-pyridyl) urea, and similar decomposition of its pyridazine analog afforded 3-(3-pyridazinyl)-2H-pyridazino [1, 6-a]-1, 3, 5-triazine-2, 4 (3H)-dione and 1, 3-di (3-pyridazinyl) urea. Aza-heteroaromatic α-isocyanates, which are intermediates in the decomposition, were utilized for the synthesis of unsymmetrical 1, 3-disubstituted ureas.

  2H-[1, 2, 4]噁二唑[2, 3-a]吡啶-2-硫酮的热分解生成了3-(2-吡啶基)-2H-吡啶[1, 2-a]-1, 3, 5-三嗪-2, 4(3H)-二酮和1, 3-二(2-吡啶基)脲，而其吡唑类似物的类似分解则生成了3-(3-吡唑基)-2H-吡唑[1, 6-a]-1, 3, 5-三嗪-2, 4(3H)-二酮和1, 3-二(3-吡唑基)脲。在分解过程中产生的氮杂杂环α-异氰酸酯被用于合成不对称的1, 3-二取代脲。