Design, Synthesis And Bioactivity Of 4-Substituted-2-phenyl-vinyl-1,3,4-oxadiazine-5-one Derivatives

The heterocyclic compounds play an important role in the research and development of pesticides owing to their high efficiencies, low toxicities and high selectivity. As a new type of sodium channel blocker combined a favorable environment profile with high activity, excellent selectivity and low residue, Oxadiazines had been applied in pesticides, medicines widely. This dissertation was made use of 1,3,4-oxadiazine-5-one as lead structure, on the basis of optimization and modification,62 novel 4-substituted-2-phenyl-vinyl-1,3,4-oxadiazine-5-one derivatives were designed and synthesized from the raw material substituted cinnamic acid. The structure of all compounds was confirmed by1H NMR and some was confirmed by GC-MS or IR.All the compounds were taken bioassay test on insect, fungi, and herb. The preliminary assays showed that some compounds exhibit certain insecticidal and fungicidal activity.The mortality of E7,E18,E19,E20,E26 to Culex pipiens pallens at the concentration of 50mg/L reached respectively 88.8%,.91.7%,,86.1%,,85.5%,,93.9%. At the same time, the inhibition of compound E2 to Sphaerotheca fuliginea at the concentration of 500mg/L reached 93.9%. The bioassay showed that all the compounds displayed poor activity toward herb.