5-乙酰基-2-糠酰氯 | 121880-45-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 呋喃
• 中文名称: 5-乙酰基-2-糠酰氯
• 英文名称: 5-acetyl-2-furoyl chloride
• 英文别名: 5-acetylfuran-2-carbonyl chloride
• CAS: 121880-45-3
• 化学式: C₇H₅ClO₃
• 分子量: 172.568
• InChiKey: KPOMYWBBXHLZEF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  11
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  47.3
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-乙酰基-2-糠酰氯 在 二甲胺 作用下， 以 四氢呋喃 为溶剂， 生成 N,N-dimethyl-5-acetylfuran-2-carboxamide
  参考文献：
  名称：

  2-guanidino-4-(2-furyl) thiazoles as antiulcer agents

  摘要：

  一系列新颖的噻唑化合物，其在2位具有胍基或取代胍基基团，在4位具有5-(N,N-二取代氨基甲基)-2-呋喃基基团。该发明的化合物可用于给哺乳动物预防或治疗消化性溃疡。

  公开号：

  US04814341A1
• 作为产物：
  描述：

  2-acetyl-5-furoic acid 在 氯化亚砜 作用下， 以 甲苯 为溶剂， 生成 5-乙酰基-2-糠酰氯
  参考文献：
  名称：

  2-guanidino-4-(2-furyl) thiazoles as antiulcer agents

  摘要：

  一系列新颖的噻唑化合物，其在2位具有胍基或取代胍基基团，在4位具有5-(N,N-二取代氨基甲基)-2-呋喃基基团。该发明的化合物可用于给哺乳动物预防或治疗消化性溃疡。

  公开号：

  US04814341A1

文献信息

• Synthesis and α1-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin
  作者：Gianni Sagratini、Piero Angeli、Michela Buccioni、Ugo Gulini、Gabriella Marucci、Carlo Melchiorre、Amedeo Leonardi、Elena Poggesi、Dario Giardinà

  DOI：10.1016/j.bmc.2007.01.028

  日期：2007.3

  alpha(1)-Adrenoceptor selective antagonists are crucial in investigating the role and biological functions of alpha(1)-adrenoceptor subtypes. We synthesized and studied the alpha(1)-adrenoceptor blocking properties of new molecules structurally related to the alpha(1B)-adrenoceptor selective antagonist (+)-cyclazosin, in an attempt to improve its receptor selectivity. In particular, we investigated the importance of substituents introduced at position 5 of the 2-furan moiety of (+)-cyclazosin and its replacement with classical isosteric rings. The 5-methylfuryl derivative (+)-3, [(+)-metcyclazosin], improved the pharmacological properties of the progenitor, displaying a competitive antagonism and an 11 fold increased selectivity for alpha(1B) over alpha(1A), while maintaining a similar selectivity for the alpha(1B)-adrenoceptor relative to the alpha(1D)-adrenoceptor. Compound (+)-3 may represent a useful tool for alpha(1B)-adrenoceptor characterization in functional studies. (c) 2007 Elsevier Ltd. All rights reserved.
• (+)-Cyclazosin Derivatives as α1-Adrenoceptor Antagonists
  作者：Gianni Sagratini、Michela Buccioni、Ugo Gulini、Gabriella Marucci、Carlo Melchiorre、Amedeo Leonardi、Rodolfo Testa、Dario Giardina

  DOI：10.1007/s00044-004-0024-8

  日期：2004.4

  The prazosin-related compound (+)-cyclazosin [(+)-1] is an (alpha(1)-adrenoceptor antagonist with moderate selectivity for the alpha(1b)-adrenoceptor subtype (selectivity ratio: alpha(1b)/alpha(1a)= 90, alpha(1b)/alpha(1d) = 24). To improve its pharmacological profile, the novel chiral derivatives (+)-2-(+)5, bearing a bromo, a methyl, a methoxy or an acetyl group in position 5 of the 2-furoyl moiety, were synthesized and evaluated for their alpha(1)-adrenoceptor blocking activity. All the compounds displayed, like (+)-1, high and preferential affinity for the alpha(1b)-adrenoceptor in binding and 4 functional assays. Interestingly, in functional assays, compounds (+)-3 and (+)-4 showed, in comparison with (+)-1, an increase in the alpha(1B)/alpha(1A) selectivity (407 and 724 vs. 44), whereas compound (+)-5 exhibited an improved alpha(1B)/alpha(1D) selectivity (1513 vs. 138).
• REITTER, LAWRENCE A.
  作者：REITTER, LAWRENCE A.

  DOI：——

  日期：——
• THIADIAZOLE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
  申请人：GRIFFIOEN Gerard

  公开号：US20090054410A1

  公开（公告）日：2009-02-26

  This invention provides specifically substituted 1,2,4-thiadiazole derivatives for use in the treatment of an α-synucleopathy such as Parkinson's disease, diffuse Lewy body disease, traumatic brain injury, amyotrophic lateral sclerosis, Niemann-Pick disease, Hallervorden-Spatz syndrome, Down syndrome, neuroaxonal dystrophy, multiple system atrophy and Alzheimer's disease. This invention also provides various methods for producing such substituted 1,2,4-thiadiazole derivatives.
• US4814341A
  申请人：——

  公开号：US4814341A

  公开（公告）日：1989-03-21