5-去氢枞基-1,3,4-噻二唑衍生物的合成和除草活性

摘要

In order to search for novel compounds with higher biological activity, a series of new dehydroabietic acid derivatives bearing 1,3,4-thiadiazole moieties were designed and synthesized. Eight title eompounds of 5-dehydroabietyl-2-substituted amino-1,3,4-thiadiazoles 5 (a-h) were synthesized by the cyclization of 1-dehydroabietacyl-4-substituted thiosemicarbazides 4(a-h) under the catalysis of phosphoric acid. All the title compounds were analyzed and characterized by means of IR, UV, EI-MS, 1H NMR, 13C NMR, and elemental analysis. The preliminary bioassay showed that all these title compounds exhibited excellent growth inhibition against rape( Brassica campestris) and a certain inhibition against barnyard grass Echinochloa crusgalli( L. ).%为了寻找具有更高生物活性的新颖化合物,设计并合成了具有1,3,4-噻二唑骨架的系列新型去氢枞酸衍生物.在磷酸催化下,通过中间体1-去氢枞酰基-4-取代基氨基硫脲4(a～h)的关环反应,合成得到8个目标产物5-去氢枞基-2-取代氨基-1,3,4-噻二唑5(a～h),并采用IR、UV、EI-MS、1H NMR、13C NMR和元素分析等方法对其进行了分析和表征.初步生物活性测试结果表明:所有这些目标化合物均对油菜(Brassica campestris)表现出良好的抑制作用,对稗草(Echinochloa crusgalli(L.))有一定的抑制活性.