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有机化学
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有机化学 ›› 1994, Vol. 14 ›› Issue (3): 293-299. 上一篇    下一篇

研究论文

含氮亲核试剂在2-甲磺酰基-5-(3,4,5-三甲氧基苯基)-1,3,4-恶二唑环上取代反应的研究

冯小明;陈荣;林涛   

  1. 中国科学院成都有机化学研究所;西南师范大学化学系
  • 发布日期:1994-06-25

Studies of nucleophilic displacements of nicleophilic agent of nitrogen on 2-methylsulphonyl-5-(3,4,5- trimethoxyphenyl)-1,3,4-oxadiazole

FENG XIAOMING;CHEN RONG;LIN TAO   

  • Published:1994-06-25

本文报道了制备2-甲磺酰基-5-(3,4,5-三甲氧基苯基)-1,3,4-恶二唑和其进一步与多种亲核试剂反应. 2-巯基-5-(3,4,5-三甲氧基苯基)-1,3,4-恶二唑经过甲基化, 而后用KMnO~4氧化得到2-甲磺酰基-5-(3,4,5-三甲氧基苯基)-1,3,4-恶二唑衍生物. 其结构由元素分析,IR, ^1H NMR 和MS确定.化合物4对大肠杆菌和枯草芽孢杆菌有较强的抑制性能.

关键词: 酰肼, 恶二唑 P, 四唑 P, 亲核取代反应, 亲核试剂, 杀菌活性

In this paper, 2-methylsulphonyl-5-(3,4,5-trimethoxyl- phenyl)-1,3,4-oxadiazole have been prepared and their subsequent transformations with a variety of nucleophilic reagents have been studied. Whereas the 2-methylsulphonyl- 5-(3,4,5-trimethoxylphenyl)-1,3,4-oxadiazole derivatives have been obtained from 2-mercupto-5-(3,4,5-trimethoxylphenyl)- 1,3,4-oxadiazole through methylation and subsequent oxidation with KMnO~4. Their structural proofs were based on elemental, IR, ^1H NMR, and MS analyses. The compounds 4 (2.0×10^-^4 mol·L^-^1) were preliminary screened for antibacterial activity against Bacillus Substilis and Escherichia Coli.

Key words: TETRAZOLE P, HYDRAZIDE, NUCLEOPHILIC REAGENTS

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