Synthesis And Bioactivity Of Novel Pyridyl-pyrazole-5-carboxylic Acid Amide Compounds

The synthesis and biological Activity of Novel 3一chloro一1一(3-chloro-2-pyridinyl)-1H-pyrazole-5-carboxylic aid amide compounds were studied in this thesis.This thesis has four chapters.The chapter one,at first recent research advances on pyridine pestic-ides were summarized detailedly.Benzene was replaced by pyridine made new compounds tend to have higher biological activity,low toxicity,high systemics or higher selectivity.It is precisely the pyridine ring in the mol-ecular design of pesticides that have such a unique effect,so these compou-nds continue to come out of pesticide products.Second,pairs of pyrazole compounds in pesticides in the study was made a detailed overview of the progress.With the pyrazole ring-substituted sites and the different substitu-ent to give the pyrazole compounds of different biological activity.Finally, the pyridine-pyrazole pesticides with the study was made a detailed over-view of the progress.The second chapter,synthesis and biological activity of novel 3-chlor-o-1-(3一chloro一2-pyridiny-1)-1H-pyrazole-5一carboxylic acid amide compou-nds were described.In this study key intermediate 3-chloro-1-(3-chloro-2-pyridinyl)一1H-pyrazole-5-carboxylic acid was synthesized starting from 2,3-dichloro-pyridine and hydrazine,which was then treated with diethyl maleate,then ester through chlorination,oxidation,hydrolysis.Carbonyl chloride was sythesized by dichloro sulfoxide,and 3-chloro-1-(3-chl-oro-2-pyridinyl)一1H-pyrazole-5一carboxylic acid ammide compounds were synthes-ized by carbonyl chloride reacting with ammonia.Intermediates and target compounds were detected and characterized.As well as the biological activ-ity of the target compounds were stu-died in detail.In the Chapter III,synthesis and biological activity of novel 3-chloro-1一(3一chloro-2-pyridinyl)一1H-pyrazole-5-carboxylic acid amide compounds were introduced.In this study key intermediate 3一chloro-1-(3-chloro-2一pyri-dinyl)-1H-pyrazole一5一carboxylic acid was synthesized starting from 2,3-dichloropyridine and hydrazine,which was then treated with diethyl malea-te,then ester through bromination,oxidation,hydrolysis.Carbonyl chloride was sythesized by dichloro sulfoxide,and 3-chloro一1一(3一chloro-2-pyridinyl) -1H-pyrazole一5一carboxylic acid ammide compounds were synthesized by carbonyl chloride reacting with ammonia.Intermediates and target compo-unds were detected and characterized.As well as the biological activity of the target compounds were studied in detail.Chapter IV,the synthesis of ethyl 1-(2,4,6一trichlorine-1-phenyl)-3一py-razolidinone一5-carboxylate,the hydrazinolysis of ethyl-3-chloro一1-(3-chlo-ro-2-pyridinyl)-1H-pyrazole一5-carboxylate and the synthesis of ethyl-3-chloro-1-(6-chloro-2-pyridinyl)-1H一pyrazole一5一carboxylate were introdu-ced respectively.The target compounds were not to be got,but the explora-tion of these synthetic routes is still very meaningful.And some synthetic methods should to be further studied and improved.