| The most important work in pesticide discovery is the finding of lead compounds. In this paper, in order to get high activities pesticide lead compounds, three types of amides were designed and synthesized.At first, two series benzoxazines A1-A16 and B1-B46 were synthesized from methyl salicylate and methyl 4-hydroxybenzoate respectively. The structures of these compounds were confirmed by 1H NMR and MS. The insecticidal activities of them were also evaluated. The results showed that B1-B46 showed favorable biological activity against Tetranychus cinnabarinus, but showed no activity against Aphisfabae Scopoli and Mythima separate at the tested concentration. At the concentration of 20 mg/L, most of the B1-B46 still show relatively high insecticidal activities against Tetranychus cinnabarinus, while compounds B12, B14, B21, B25, B30 exhibited more than 50% mortality against Tetranychus cinnabarinus at the concentration of 4 mg/L.Second, according to the research on flubendiamide, chlorantraniliprole and other related patents, a series of novel 3-acylaminobenzamides containing heptafluoroisopropyl moiety were synthesized. The structures of these products were confirmed by 1H NMR and MS. The insecticidal activities of them were also evaluated.The bioassay results showed that these compounds have moderate activities. It was worthy noting that, at the concentration of 4 mg/L, compound C10 showed 100% mortality against Plutella xylostella and it could be a potential lead compound for further research.At last, with m-nitrobenzoic acid as raw material, a series of novel phenyl urea compounds D1-D40 containing heptafluoroisopropyl were synthesized by introducing active moiety of heptafluoroisopropyl aniline. The structures of these products were confirmed by 1H NMR and MS, and the insecticidal activities of them were also determined. The bioassay results showed that some compounds showed about 80% mortality against Plutella xylostella at the concentration of 500 mg/L. |
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