将5-取代吡唑-3-甲酸乙酯1位甲基化,经水解反应得到3种中间体l-甲基-5-取代-1H-吡唑-3-甲酸(2a~2c);以不同取代的羧酸为原料经一系列反应合成6种中间体3-取代4-氨基-5-巯基-1,2,4-均三唑(3a~3f);将中间体(2a ~2c)和(3a~3f)在三氯氧磷条件下反应,合成出18种1,2,4-三唑并[3,4-b]-1,3,4-噻二唑类化合物(4a ~4r),均未见文献报道.通过IR、1H NMR、13C NMR和元素分析表征了化合物结构.初步的生物活性测试结果显示,所合成的化合物均表现出不同程度的生长素活性和抑菌活性.并选取抑菌活性较好的两个化合物进行抗菌药物最低抑菌浓度(MIC)的测定.
参考文献
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