Studies On Design,Synthesis And Properties Of 5-pyrazole Carboxylic Acid Derivatives

High efficiency,low toxicity and safety are the theme of pesticide research nowadays.Pyrazole compounds play an important role in agricultural field which have high efficiency,broad-spectrum biological activity and transform the diversity of substituents in the pyrazole ring.Studies on design,synthesis and biological activities of pyrazole compounds have been one of the research direction of green agrochemicals.This paper reviewed the development situation,classification and development trend of pesticide.The latest research progress of pyrazole agrochemicals were introduced detailedly.In this paper unreported and novel 5-Pyrazole carboxylic acid derivatives were designed and synthesized by analogue synthesis,sub-structure and intermediate derivatization methods.According to the structure,the target compounds can be divided into the following categories:Synthesis methods for target compounds and involved intermediates were studied.The structures of newly synthesized compounds were confirmed by NMR,MS and IR spectra.The insecticidal,acaricidal,fungicidal,herbicidal activities of these compounds were evaluated by bioassay procedure.The insecticidal activity bioassay results showed that compounds I exhibited significant effect against Aphis fabae,Mythimna separate,and Tetranychus urticae at the concentration of 500 mg/L,such as compounds 12,14,I11 and 112 against Aphis fabae with 90.0%death rate,compound 16 againstMythimna separate with 100.0%death rate and compound 12 against Tetranychus urticae with 100.0%death rate.The fungicidal activity bioassay results showed that the compounds I1,I2 exhibited good fungicidal activities against Blumeria graminis with 90.0%inhibition rate and compound 117 exhibited good fungicidal activities against Puccinia polysora with 90.0%inhibition rate at the concentration of 500 mg/L.The herbicidal activity bioassay results showed that the compounds 13,15,113,114 exhibited different degrees of herbicidal activities against Digitaria sanguinalis,Amaranthus spinosus and Chenopodium album at the dosage of 2250 g a.i/ha,such as compounds 13,15 against Digitaria sanguinalis with 70.0%activities by soil treatment,compounds 113,114 against Chenopodium album with 70.0%activities by foliage treatment.Most of the compounds had no herbicidal activities.The structure-activity relationship based on bioactivity of the target compounds were discussed.The conclusion which was summarized can provide some theoretical guidance for designing such compounds in future.