Synthesis Of Fluopicolide Analogues And Study Of The Biological Activity

Pesticides are of great significance to the development of agriculture.In order to find new green,high efficiency and low toxicity pesticides,this paper,based on the summary of a large number of relevant literature,designed and synthesized 71 compounds,including 22 amino acid esters and 49 pyrimidazole compounds and their derivatives,using the intermediate-derived method and taking fluopicolide as the lead compound.The structure of the compound was determined by 1H NMR,LC-MS,IR and XRD,and the bioactivity was measured.Based on the intermediate 2-[(3-chloro-5-trifluoromethyl)pyridine]glycine ester,a series of amino acid esters were synthesized by using the substitution method in the intermediate derivation method.It was found that the newly synthesized amino acid esters had not only bactericidal activity but also insecticidal activity.At a dose of 600 mg/L,the lethal activity of compound M-22 against diamondback moth was 100%,and that of compound M-1 and M-2 against wheat powdery mildew was 100%at a dose of 400 mg/L.Other compounds also showed a certain degree of insecticidal and bactericidal activity,which has potential research value.Novel pyrimidazole structure compounds and their derivatives were obtained by using fluopicolide analogues under the action of phosphorus trichloroxide.The biological activity tests showed that the pyrimidazole compounds had insecticidal,weeding and bactericidal activities.At the dose of 600 mg/L,the pyrimidazole compounds had insecticidal activities against diamondback moth,armyworm and myzus persicae,and the insecticidal activities of most compounds were 100%.At the dose of 1000 g a.i./hm2,pyrimidazole series compounds had herbicidal activities against zinnia grass,abutilon,hackweed and barnyard grass,among which compound IP-18 had herbicidal activities against the above four targets of 80%,85%,90%and 85%,respectively.At the dose of 400 mg/L,some pyrimidazole compounds had good control effects on cucumber downy mildew,wheat powdery mildew and corn rust.