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为研究鬼臼毒素类化合物结构与杀虫活性的关系,设计合成了3个4β-卤代-4-脱氧鬼臼毒素和4个4β-氨基-4-脱氧鬼臼毒素类化合物,通过IR、M S1、H NMR和元素分析对其结构进行了确证。采用小叶碟添加法测试了合成化合物对3龄粘虫M ythimna separate幼虫24h和48h的拒食活性,结果表明:4β-卤代-4-脱氧鬼臼毒素类化合物的活性相对高于氨基取代产物、母体化合物鬼臼毒素和对照品脱氧鬼臼毒素,其中4β-溴代-4-脱氧鬼臼毒素活性最高,其对粘虫幼虫24h和48h的AFC50分别为280.8和392.9mg/L,分别是母体化合物鬼臼毒素的3.43和1.90倍,是对照品脱氧鬼臼毒素的2.46和1.57倍;4β位引入氨基活性降低,4β-叠氮衍生物的活性最低。
In order to study the relationship between the structure of podophyllotoxins and pesticidal activity, three 4β-halo-4-deoxypodophyllotoxins and four 4β-amino-4-deoxypodophyllotoxins were designed and synthesized. Their structures were characterized by IR, Its structure was confirmed by M S1, H NMR and elemental analysis. The antifeedant activity of the synthesized compounds against the 3rd instar M. armigera larvae 24h and 48h was tested by using the leaf disc addition method. The results showed that the activity of the 4β-halo-4-deoxypodophyllotoxins was relatively higher than that of the amino-substituted products, The parent compound podophyllotoxin and reference substance deoxypodophyllotoxin, among which 4β-bromo-4-deoxypodophyllotoxin had the highest activity, and its AFC50 against armyworm larvae at 24h and 48h were 280.8 and 392.9mg / L, respectively, 3.43 and 1.90 folds of the compound podophyllotoxin were 2.46 and 1.57 folds of that of the control podophyllotoxin. The amino group activity of 4β-adrenoceptor decreased and the activity of 4β-azide derivatives was the lowest.