Synthesis and activity of spinetoram derivatives

Abstract

As the second generation commercial product of spinosyns, spinetoram not only has obvious insecticidal effect on vegetable crops, but also can effectively control pests on fruits and nuts. It has been widely used in pest control. In order to find more efficient insecticides, a series of spinetoram derivatives were synthesised. The structures were confirmed by 1H NMR,13C NMR and HRMS, and the insecticidal activity of these derivatives against Plutella xylostella was determined. The insecticidal activity of derivatives against P. xylostella was better than that of the commercially available dihydrazide insecticides. Through the preliminary analysis of the structure-activity relationship of spinetoram derivatives, it was found that the introduction of electron-withdrawing substituents was more likely to produce spinosad compounds with high insecticidal activity, but the position of the substituent had little effect on the insecticidal activity, which was of great significance for the future study of spinetoram derivatization.