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为寻找具有优良杀菌活性的吲哚衍生物,以吲哚等为原料利用Vilsmeier反应制得3-乙酰吲哚,然后经过羟醛缩合、加成-消除反应合成了一系列新型含吲哚环的2-丙烯-1-酮肟醚3a～3j,其结构通过IR,1H NMR,ESI-MS和元素分析确证.用生长速率法测试了目标化合物对番茄灰霉菌和西瓜炭疽菌的离体抑菌活性,结果表明化合物对两种病原菌有一定的抑制活性,其中3f和3g对番茄灰霉菌抑制活性较高,在浓度为100μg/mL时抑制率分别为81%和74%.
In order to search for indole derivatives with excellent bactericidal activity, 3-Acetylindole was synthesized by Vilsmeier reaction using indole as starting material, and then a series of novel indole ring-containing compounds were synthesized via aldol condensation and addition-elimination reaction The structures of the compounds were confirmed by IR, 1H NMR, ESI-MS and elemental analysis. The growth inhibition method was used to test the in vitro inhibition of the target compounds against Botrytis cinerea and watermelon anthrax The results showed that the compounds had certain inhibitory activity against two kinds of pathogens. Among them, 3f and 3g showed high inhibitory activity against Botrytis cinerea, and the inhibitory rates were 81% and 74% at the concentration of 100μg / mL respectively.