Synthesis And Bioactivity Of Novel Pyrimidine Compounds

Pyrimidine compounds have excellent insecticidal,bactericidal and acaricidal activities,and are widely used in modern pesticides and medicines,so they have become one of the hot spots in the creation of new pesticides.In order to develop pyrimidine compounds with high activity,in this paper,fluacrypyrim was used as the lead compound,and five pyrimidine analogs were designed and synthesized by the intermediate derivatization method;using azoxystrobin as the lead compound,33fluoropyrimidine sulfide compounds were designed and synthesized by active substructure splicing method;Using ethyl ethoxymethylene cyanoacetate and thiourea as starting materials,10 pyrimidine amine derivatives were designed and synthesized by active substructure splicing method.Three types of 48 target compounds were synthesized and characterized by ~1H NMR,¹³C NMR and HRMS.The synthesis methods of some target compounds were reasonably optimized,and the best synthesis method was put forward.The insecticidal,bactericidal and acaricidal activities of the relevant target compounds were determined according to indoor biological activity test standards.In terms of activity against diamondback moth,three pyrimidine analogs in series II,one pyrimidine sulfide compound in series III1,and one pyrimidineamine compound in series IV2 and series IV3 each showed excellent efficacy against diamondback moth.Biological activity,among which the lethality rate of compound III1-m to diamondback moth was 97%at the concentration of 1 mg/L,showing the best biological activity in the aspect of diamondback moth;in terms of sterilization,there are some compounds in series III2 and III3 It showed moderate inhibitory activity;in terms of acaricidal activity,one pyrimidine sulfide compound in each of series III2 and III3 showed excellent acaricidal activity,Among them,the lethality rate of compoundⅢ3-c to Tetranychus cinnabarinus was 100%at 1 mg/L.Therefore,some of the target compounds synthesized not only exhibit excellent biological activities,but also have novel structures,which are worthy of further exploration.