New Neonicotinoid Synthesis And Insecticidal Activity Was Measured (b)

The discovery of neonicotinoid insecticides (NNs) can be considered as a milestone in agrochemical research over the past three decades because of its advantages, such as, high insecticidal potency, safety, high selectivity.Ⅰn order to find some lead compounds with insecticidal activities and search the introduction compounds for new pesticide, a total of two series of 18 unreported compounds shown in the formula (Ⅰ) and (Ⅱ) were designed and synthesized. A series of seven novel neonicotinoids analogues alkylene-tethered bis-nitenpyram(Ⅰa-Ⅰg)were designed by linking two nitenpyram molecules with various alkyl chains. A series of eleven novel neonicotinoids analogues 1,5-disubstituted-1,3,5-hexahydrotriazine-2-N-nitroi-mines (Ⅱa-Ⅱk)were synthesised by mannich reaction. All these target compounds are new compounds and their structures were confirmed by 1H NMR,ⅠR, elementary analysis, and LC-MS. Their physic-chemical properties, spectrum properties, reaction conditions and synthetic methods were discussed as well.The preliminary biological activities tests of target compounds (Ⅰ), (Ⅱ) were finished in Zhejiang ChemicalⅠndustry ResearchⅠnstitute. The German Bayer CropScience Company helped us to test the insecticidal activity of compounds (Ⅰ).The preliminary biological activities tests shows target compounds (Ⅰ) have some insecticidal activities against Nilaparvata legen. Especially, the compoundⅠd afforded the best in vitro inhibitory activity, and had > 60% mortality 1.2 mg/L. Target compounds (Ⅱ) have good insecticidal activities against Tetranychus cinnabarnus at 500mg/L, the compoundⅡa andⅡj had≥90% mortality 500 mg/L. The physic-chemical properties, spectrum properties, reaction conditions and synthetic methods of target compounds were discussed. Their structure-activity relationship were also discussed.