Synthesis And Biological Activity Of Pyridine Substituted Pyrazole Acetic Acid Derivatives

Recently nitrogen-containing heterocyclic ring such as pyridine and pyrazole compounds have been used to research and develop pesticides lead compounds for their extensive biological activity and unique mechanism of action.To discover new pesticide lead compounds with higher biological activities,84 novel pyridyl substituted pyrazole carboxylic acid derivatives were designed and synthesized by introducing substituted anilines,5-substituted-1,3,4-thiadiazol-2-amine,phenoxyacetyl amino hydrazine to pyridyl substituted pyrazole carboxylic acid structure,according to the splicing principle of active substructures,and their structures were characterized by ~1HNMR,MS,IR,also the biological activities of some compounds were evaluated preliminarily.The main contents of this thesis involved are listed as follows:1.The intermediates of pyridyl substituted pyrazole acid were synthesized from substituted pyridine,acetylacetone and ethyl bromoacetate after several reactions of alkylation,cyclization,hydrolysis,acidification and condensa-tion,then use these intermediates as parent structures,and spliced them with substituted aniline,5-substituted-1,3,4-thiadiazol-2-amie and substituted hydrazides according to the splicing principle of active substructures,resultly,totally 84 compounds of amides and diacylhydrazines were synthesized.2.The biological activities of some compounds were evaluated,the results showed that some compounds exhibit a variety of biological activities due to their different substituents,for example,compound A1,A5,A8,B7,B11 exhibited good insecticidal activity;Compound A3,A4,B3,B4 showed good control effect to Erisiphe griminis,whose bactericidal activity was similar to trifloxystrobin;Compound A5,B2,B6 exhibited 100%inhibition rate to Abutilon theophrasti Medicus,Amaranthusretroflexus,Amaranthus lividus L,their herbicidal activity are similar to grass isopropyl ether.