| Acrylonitrile compounds and pyrazole amide compounds have excellent acaricidal,insecticidal and bactericidal activities and are widely used in pesticides and medi-cines.Due to the unique advantage of pyridyl and pyrazole carboxylic acid deriveatives in pesticide intermediates,it has become one of the focuses of new pesticides.In order to develop a highly active compound,three 1-arylpyrazole-5carboxylic acids and one 1-ethylpyrazole-5-carboxylic acid were designed and synthesized,using 3-br-omo-1-(3-chloropyridin-2-yl)-1H-pyrazole-5-carboxylic acid as a lead compound.Ei-ght pyrazole-containing acrylonitrile compounds were synthesized using cyenopyrafe-n as a lead compound.Ten 1-arylpyrazoles-5-amide compounds were synthesized from tebufenpyrad,tolfenpyrad and chlorantraniliprole by using similar synthesis and active substructure splicing method.In addition,five fipronil amide derivatives were synthesized,and the optimal synthesis process of compound ?-2d were determined.Nine dehydrotetrahydrofuran derivatives were synthesized from cantharidin as matrix.Four types of 32 target compounds were synthesized and the structure of the target compounds were determined by means of ~1H NMR,HRMS and GC-MS.The acaricidal,insecticidal and bactericidal activities of the relevant compounds were determined according to the indoor biological activity test standard.Among the-m,eight acrylonitrile compounds,six 1-arylpyrazole-5-amide compounds and one ca-ntharidin analogy showed better acaricidal activity.Six 1-arylpyrazole-5-amide comp-ounds and five fipronil derivatives also showed activity against Plutella xylostlla.At the concentration of 0.1 mg/L,the lethal rate of compound ?5-2c against Plutella xylostella reached 87.9%.Although the dehydrotetrahydrofuran derivatives have a certain bactericidal activity,the effect is not outstanding.Among them,compound 3-9both has acaricidal and insecticidal activity,and its structure is novel,so it has the value of continued development. |
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