摘要/Abstract

为了寻找高活性农药先导化合物，以甲霜灵为先导，通过活性基团拼接原理，设计合成了一系列未见文献报道的双酰胺类化合物，其结构经¹H NMR、¹³C NMR和HRMS表征.初步的生物活性测试结果表明：在50 mg/L测试浓度下，化合物5j对黄瓜霜霉病显示出85%的抑制率；在500 mg/L剂量下，多数目标化合物对粘虫表现出较好的杀虫活性，其中化合物5b，5f，5g，5h，5i，5l对粘虫的致死率高达100%，在250 mg/L测试浓度下，化合物5f，5h，5l对粘虫的致死率为50%.
关键词: 双酰胺类化合物, 合成, 生物活性
In order to find pesticidal lead compounds with high activity, a series of novel diamide compounds were designed and synthesized by using metalaxyl as a leading compound, as well as the principle of active substructure combination. The structures of the target compounds were confirmed by ¹H NMR, ¹³C NMR and HRMS. The preliminary bioassay showed that compound 5j showed an 85% inhibition rate against Pseudoperoniospora cubensis at 50 mg/L, most of the target compounds had good insecticidal activity against Oriental armyworm at 500 mg/L, and compounds 5b, 5f, 5g, 5h, 5i and 5l have a mortality rate of 100% against Oriental armyworm. At 250 mg/L, the mortality rate of compounds 5f, 5h and 5l against Oriental armyworm was 50%.
Key words: diamide compound, synthesize, biological activity


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