Synthesis And Biological Activities Of Pyrazole Carboxylic Acid Derivatives

Recently diacylhydrazines acyl thiosemicarbzides and amide compounds are widely studied and used in the green pesticide fields in order to find out novel pesticide lead compounds for their good biological activities.Because pyrazole compounds have good biological activities.Pyrazole acids were used as main group to synthesize series of acylthiourea diacylhydrazines and thiadiazols amide compounds.Totally 116 novel target compounds were obtained.Their structures were confirmed by 1H NMR and MS.The biological activities of these compounds were evaluated.The main contents are listed as follows:1.The corresponding esters were obtained by reaction with substituted phenols and ethyl chloroacetate,and 45 diacylhydrazines compounds were got by the condensation reaction between pyrazole acid chloride and different substituted hydrazide.At the concentration of 200 mg/L,The Herbicidal activities results showed that A12 had strong inhibitory against 6 kinds of test target of the root/stem growth effect.The fungicidal activities were also evaluated.The fungicidal activities results showed compounds C1 showed the same effect of mortality against Cucumber mould.2.31 pyrazole acylthioureas were synthesized by the carboxylate reaction,chlorination reaction and addition reaction from Pyrazole acids and substituted hydrazides as the raw materials.3.Thirteen 5-substitued-2-amine-1,3,4-thiadiazols were obtained by using substituted acids and thiosemicarbazide,and then 40 thiadiazol amide compounds were synthesized from substituted thiadiazol amines and pyrazole chloride.4.The target compounds were confirmed by 1HNMR,MS and initially tested biological activity.