Syntheses And Antifungal Activity Of Noval Trizaole Compounds(Ⅲ)

In the progress of looking for the new fungicide,triazole compounds have been paid more attention because of its wide spread biological activities,many of which have been developed and applied as fungicides,insecticides,plant growth regulator and drugs.Triazole compounds of different structures have different biological activity,and developing new type of this compound becomes a research focus at present.As the most important part of pesticide-The triazole compounds have the fastest development and the maximum number others don't have,only because of their power aspiration,lower toxicities to people and livestocks and longer residual effects.As an important part of triazole fungicides,triazolone compounds have been found from their application in China that,it not only is a broad-spectrum and highly effective fungicide,but also have good combating effect for kinds of microbicides in food crops and cash crops.In this papper,we use theα-trizaole pinacolone(3,3-dimethyl-1-(1H-1,2,4-triazol-1-yl) butan-1-one) as raw materials,the intermediatesâ… (α,β-unsaturated ketones) was prepared from different substituted benzaldehyde and 3,3-dimethyl-1-(1H-1,2,4-triazol-1-yl) butan-1-one through the aldol condensation reaction with piperidine as catalyst reflux in benzene,the intermediatesâ…¡was obtainted by the reaction of compoundâ… with morpholine or pentane-2,4-dione,some compounds ofâ…¡(â…¡b-â…¡d) then have the reduction reaction by NaBH₄ or have the oximation reaction by NH₂HCl with methanol as solvent,finally we get 12 compounds which have the triazole's structure,and 8 of them belongs to ketones,3 of them belongs to alcohols and 1 is oximes.Their structures were confirmed by means of ¹H NMR,IR and Ms,several were confirmed by ¹³C NMR.The preliminary result of bacteriostasis activities indicated that most of these compounds have some biological activities for plant pathogenic bacterium under the concentration of 100 mg/L.In general,compounds contains the structure of ketone have better biological activities than contains alcohol structure,and compounds have strong Electron-Withdrawing group better than have Electron-Donating group.