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有机化学
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有机化学 ›› 2012, Vol. 32 ›› Issue (07): 1336-1339.DOI: 10.6023/cjoc1111271 上一篇    下一篇

研究简报

5-磷酰基-3-芳基异噁唑啉的合成及结构表征

张长水a, 叶勇b   

  1. a 河南科技大学 化工与制药学院 洛阳 471003;
    b 郑州大学 化学系 河南省磷化工工程技术研究中心 郑州 450052
  • 收稿日期:2011-11-27 修回日期:2011-12-30 发布日期:2012-03-31
  • 通讯作者: 叶勇 E-mail:yeyong@zzu.edu.cn
  • 基金资助:
    国家自然科学基金(No. 20972143)资助项目.

Synthesis and Characterization of 5-phosphonyl 3-arylisoxazoline

Zhang Changshuia, Ye Yongb   

  1. a Chemical Engineering & Pharmaceutics College, Henan University Of Science & Technology, Luoyang 471003;
    b Phosphorus Chemical Engineering Research Center of Henan Province, Department of Chemistry, Zhengzhou University, Zhengzhou 450052
  • Received:2011-11-27 Revised:2011-12-30 Published:2012-03-31
  • Supported by:
    Project supported by the National Natural Science Foundation of China (No. 20972143).

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本文通过乙烯基膦酸酯与氧化腈的环加成反应,合成了一系列区域专一的异噁唑啉,化合物3c 的单晶X衍射证实产物为5-磷酰基异噁唑啉。目标化合物结构经核磁、电喷雾质谱和元素分析表证,生物活性测试表明这些化合物具有一定的神经氨酸酶抑制活性。

关键词: 乙烯基膦酸酯, 氧化腈, 环加成反应, 异噁唑啉

A series of regioselectively isoxazolines were synthesized through cycloaddition reaction of nitrile oxides with vinylphosphonate. The structure of title compound was proved as 5-phosphonyl isoxazoline by X-ray crystallography of compound 3c. Their structures were confirmed by NMR, ESI-MS and elemental analysis. We have tested suppression of the NIs, and found they can inhibit neuraminidase.

Key words: Vinylphosphonates, nitrile oxides, 1,3-Dipolar cycloadditions, isoxazoline