1-(2-Furyl)phthalazin-4(3H)-one | 97694-84-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 1-(2-Furyl)phthalazin-4(3H)-one
• 英文别名: 4-(2-furyl)-1-phthalazinone；4-(furan-2-yl)-2H-phthalazin-1-one
• CAS: 97694-84-3
• 化学式: C₁₂H₈N₂O₂
• 分子量: 212.208
• InChiKey: PPPVYZSHYRMUFJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  54.6
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-(2-Furyl)phthalazin-4(3H)-one 在 sodium hydride 、 sodium carbonate 、 sodium iodide 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 3.0h， 生成 N-[3-[1-[3-[4-(furan-2-yl)-1-oxophthalazin-2-yl]propyl]piperidin-4-yl]phenyl]acetamide
  参考文献：
  名称：

  4-Heteroaryl Phthalazin-1(2H)-one Derivatives as Potent Melanin Concentrating Hormone Receptor 1 (MCH-R1) Antagonists

  摘要：

  DOI：

  10.5012/bkcs.2012.33.7.2389
• 作为产物：
  描述：

  2-(2-furoyl)benzoic acid 在 一水合肼 作用下， 以 乙醇 为溶剂， 生成 1-(2-Furyl)phthalazin-4(3H)-one
  参考文献：
  名称：

  3,6-disubstituted pyradazine derivatives

  摘要：

  一种具有出色的血小板凝聚抑制作用的3,6-二取代吡啶嗪衍生物。它可用于预防或治疗脑血栓和脑栓塞等脑血管疾病，心肌梗死等缺血性心脏病以及外周循环障碍等循环系统疾病的预防性或治疗性药物。本发明还公开了一种含有该化合物作为有效成分的制药组合物以及其制备方法。该化合物的化学式为（I）其中，A代表具有3到6个碳原子的烷基；具有5到7个碳原子的环烷基；苯基，噻吩基，呋喃基，噻唑基，苯氧基，具有7到9个碳原子的苯基烷基，苯硫基，含有一个或多个氮原子的5-6成员饱和杂环基，吡啶基或咪唑基，其中每个基团都可以具有至少一个选自由1到4个碳原子的烷基，1到4个碳原子的烷氧基和卤素原子的取代基；B代表（a）--NH--D，其中D代表##STR2##（4）--CH3R4；或（5）具有3到8个碳原子的烷基；或##STR3##环C代表苯环。

  公开号：

  US05462941A1

文献信息

• 3,6-disubstituted pyradazine derivatives
  申请人：Mitsubishi Chemical Corporation

  公开号：US05462941A1

  公开（公告）日：1995-10-31

  A 3,6-disubstituted pyridazine derivative having excellent platelet agglutination inhibitory effects. It is useful for a preventive medicine or a therapeutic medicine for a cerebrovascular disorder such as cerebral thrombosis and cerebral embolism, an ischemic heart disease such as myocardial infarction, and a circulation disorder such as peripheral circulation disorder. A pharmaceutical composition containing a compound of the present invention as an effective ingredient and a process for preparing the same are also disclosed. The compound has the formula (I) ##STR1## wherein A represents an alkyl group having 3 to 6 carbon atoms; a cycloalkyl group having 5 to 7 carbon atoms; a phenyl group, a thienyl group, a furyl group, a thiazolyl group, a phenoxy group, a phenylalkyl group having 7 to 9 carbon atoms, a phenylthio group, a 5-6 membered saturated heterocyclic group containing one or more nitrogen atoms, a pyridyl group or an imidazolyl group each of which may have at least one substituent selected from the group consisting of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms and a halogen atom; B represents (a) --NH--D wherein D represents ##STR2## (4) --CH.sup.3 R.sup.4 ; or (5) an alkyl group having 3 to 8 carbon atoms; or ##STR3## and the ring C represents a benzene ring.

  一种具有出色的血小板凝聚抑制作用的3,6-二取代吡啶嗪衍生物。它可用于预防或治疗脑血栓和脑栓塞等脑血管疾病，心肌梗死等缺血性心脏病以及外周循环障碍等循环系统疾病的预防性或治疗性药物。本发明还公开了一种含有该化合物作为有效成分的制药组合物以及其制备方法。该化合物的化学式为（I）其中，A代表具有3到6个碳原子的烷基；具有5到7个碳原子的环烷基；苯基，噻吩基，呋喃基，噻唑基，苯氧基，具有7到9个碳原子的苯基烷基，苯硫基，含有一个或多个氮原子的5-6成员饱和杂环基，吡啶基或咪唑基，其中每个基团都可以具有至少一个选自由1到4个碳原子的烷基，1到4个碳原子的烷氧基和卤素原子的取代基；B代表（a）--NH--D，其中D代表##STR2##（4）--CH3R4；或（5）具有3到8个碳原子的烷基；或##STR3##环C代表苯环。
• Wharton, Clifford J.; Wrigglesworth, Roger, Journal of the Chemical Society. Perkin transactions I, 1985, p. 809 - 814
  作者：Wharton, Clifford J.、Wrigglesworth, Roger

  DOI：——

  日期：——
• Novel antiasthmatic agents with dual activities of thromboxane A2 synthetase inhibition and bronchodilation. 1. 2-[2-(1-Imidazolyl)alkyl]-1(2H)-phthalazinones
  作者：Masahisa Yamaguchi、Kenshi Kamei、Takaki Koga、Michitaka Akima、Toshio Kuroki、Nobuhiro Ohi

  DOI：10.1021/jm00077a008

  日期：1993.12

  A number of 4-substituted 2-[omega-(1-imidazolyl)allryl]-1(2H)-phthalazinones were synthesized in order to develop agents possessing both thromboxane Az synthetase inhibitory and bronchodilatory activities. The pharmacological evaluation of these compounds disclosed that they have both activities to various extents. Both activities were slightly dependent on the length of the 2-substituents and largely affected by the nature of the 4-substituents. Compounds bearing phenyl and thienyl groups exhibited relatively high and well-rounded activities. Among these compounds, 12j and 15f were found to be the most effective agents having well-rounded activities in vitro and in vivo. Introduction of a carboxyl group reduced both activities contrary to our expectation. 4-(3-Pyridyl)phthalazinone 18b was of particular interest because of unexpectedly high in vivo activities in spite of an absence of significant in vitro activities.
• WHARTON, C. J.;WRIGGLESWORTH, R., J. CHEM. SOC. PERKIN TRANS., 1985, N 4, 809-813
  作者：WHARTON, C. J.、WRIGGLESWORTH, R.

  DOI：——

  日期：——
• 3,6-Disubstituted pyridazine derivatives
  申请人：Mitsubishi Chemical Corporation

  公开号：EP0534443B1

  公开（公告）日：1998-12-30