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 ,
  • 叶勇
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  • 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

  网络出版日期: 2012-03-31

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 Changshui ,
  • Ye Yong
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  • 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 date: 2011-11-27

  Revised date: 2011-12-30

  Online published: 2012-03-31

Supported by

Project supported by the National Natural Science Foundation of China (No. 20972143).

摘要

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。

本文引用格式

张长水 , 叶勇 . 5-磷酰基-3-芳基异噁唑啉的合成及结构表征[J]. 有机化学, 2012 , 32(07) : 1336 -1339 . DOI: 10.6023/cjoc1111271

Abstract

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.

参考文献

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