Design,Synthesis And Biological Activity Of Fluorine-containing Amides

Pyrazole amide derivatives and quinoline amide derivatives have been widely used in pesticide field.Due to the special characteristic of fluorine atom,such as simulative,electronic,obstructive and osmotic fuction,increase biological activities.Therefore,fluorine-containing pesticide is becoming a hot spot.In this paper,two types of fluorine-containing amide derivatives were designed and synthesized,in order to discover high active pesticide pilot structure.The 16 novel difluoromethyl substituted pyrazole amide derivatives were synthesized with nucleophilic substitution,cyclization,hydrolysis and addition reaction using ethyl 4,4-difluoro-3-oxobutanoate and triethoxymethane as raw materials.The structures of the compounds were confirmed by MS and 1H NMR.Two series Fluorine-containing quinolinic acid were synthesized from 5-chloroisatin and substituted acetophenone.The 77 novel quinoline amide derivatives were synthesized with acyl chlorination.The structures of these compounds were confirmed by 1H NMR and MS.The target compounds initially tested biological activity,and their structure-activity relationship was studied.The bioassay results of biological activities showed that some of the compounds ehibited good fungicidal activities.