Study On Synthesis, Properties And Bioactivities Of Propiconazole-Metal Complexes

Propiconazole was developed by Giba-Geigy Co., a Switzerland company in 1979, it was one of triazole fungicides applied on a large scale. It can be used to prevent plant diseases caused by Ascomycetes, Basdiomycetes and Deuteromycetes, especially Fusarim graminearum schw., Erysiphe graminis and Fussrium moniliforme. But the germination of seeds by propiconazole was generally considerably reduced, so it was forbided to be applied to seeds. The objectives of the present work were to study on synthesis, properties and bioactivities of propiconazole-metal complexes in order to improve properties of propiconazole, to expand scope of its application and to exploit new formulation which will be more safe to environment.The thesis includes three parts:In part one: Study on Preparation and Crystal Structure of Cis-propiconazolePotent bioactivity of propiconazole is relative to its complicated molecular configuration. Its structure contains four enantiomers including cis-racemate and trans-racemate for two chiral carbon atoms on its dioxolane. The four pure enantiomers exhibit difference levels of activities as foliar fungicides and can be placed in the following order according to the degree of their activities : 2S,4R > 2S,4S > 2R,4S > 2R,4R. The cis-racemate contains a pair of enantioners having the 2S,4R- and the 2R,4S- configuration, and the trans-racemate contains a pair of enantioners having the 2S,4S- and the 2R,4R-configuration. In a word, the cis-racemate can show a higher protective activity against fungi than the Trans-racemate. So it is importent to prepare and determine stereomeride of propiconazole in order to research structure activity relationships of different isomers of propiconazole. Cis-propiconazole was prepared by forming salt with nitric acid and silica gel column chromatography, its structure was determined by X-ray diffraction analysis. The single crystal belongs to monoclinic system with space group P2₁/c, a = 1.0653(3) run, b = 1.8940(6) nm, c = 0.8104(3) nm, β= 100.032(6)°, Z = 4, V = 1.6100(9) nm³, Dc = 1.412...