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

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.

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

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.