Study On Synthesis And Biological Activity Of Acrylonitrile Compounds

The trend of future pesticides is efficient,low toxicity and residue,readily biodegradable and safe for non-target organisms.Thiazole compounds had become a hot field in green agrochemicals,because of theirstrong structural derivatives,highbiologicalactivity,broad-spectrum,low toxicity in various characteristics.Due to the novel structure,high activity,low toxicity on mammals and fish and no cross-resistance with existing insecticides,acrylonitrile compounds have attracted widespread attention at the same time.Thiazolyl acrylonitrile compounds which had framework of both thiazole and acrylonitrile have attracted more and more concern to the majority of researchers.In this paper,NC-510 as the lead compound,novel thiazolyl acrylonitrile compounds were designed and synthesized by pro-drug,sub-structure and bioisosterism theory,while the thiazole ring and acrylonitrile structure were modificated and optimized.The detail was listed as follow.1.This paper reviewed the classification and the development trend of insecticides and introduced the research progress of acrylonitrile compounds in detail.2.Two series of novel thiazolyl acrylonitrile compounds?,?were synthesised.(1)3-(4-(trifluoromethyl)thiazol-5-yl)acrylonitrile compounds?;(2)3-(4-methyl-thiazol-5-yl)acrylonitrile compounds?.(?)3.Their structures of all target compounds were confirmed by using IR,~1H NMR and LC-MS.Synthetic methods of intermediate 3 and intermediate 10 were discussed and the reaction conditions were optimized.(?)4.Biological activities of the compounds synthesized were tested.The results showed that most compounds possessed excellent insecticidal and acaricidal activities,certain fungicidal activities,no herbicidal activities completely.Compound?2 exhibited 100%mortality rate against Mythimna siparata,Aphis fabae and Tetranychus urticae at a concentration of 50 mg/L and more than 90%control effect against Rhizoctonia solani and Corn rust at a concentration of 500 mg/L.5.The structure-activity relationship based on biological activity for the target compounds was discussed.The law which was summarized can provide some theoretical guidance for designing such compounds in the future.