双酰胺类化合物的合成及生物活性研究

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,51对粘虫的致死率为50%.

Synthesis and Biological Activity of Diamide Compounds

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 combi nation.The structures of the target compounds were confirmed by*H NMR,13C NMR and HRMS.The preliminary bioassay showed that compound 5j showed an 85%inhibition rate against Pseudoperoniospora cube ns is 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 51 have a mortality rate of 100% against Oriental armyworm.At 250 mg/L,the mortality rate of compounds 5f,5h and 51 against Oriental armyworm was 50%.