Study On The Synthesis And Biological Activity Of Novel Fluorine-Containing Triazole Compands And The Synthetic Technology Of Acibenzolar

Triazole compounds have been found to show wide spread biological activities. Many of them have been developed and used as fungicides, plant growth regulators and medicine. Different structures of triazole compounds have different biological activities, developing novel structural triazole compounds is the research focus at present.In this paper, the developing survey, action mechanism, structure-activity relationship and biological activities of triazoles are reviewed. By use of the epoxidation, ten novel triazole compounds have been designed and synthesized. The structures are listed as follows:Their structures were confirmed by means of EA, IR, 1H NMR, and MS. The spatial configurations were studied by X-ray determination (two single crystals of these compounds were obtained). The results of premliminary biological tests show that all of these compounds possess good antifungal activities, some of which have high potential developing value as novel fungicide.Plant activator acibenzolar-S-methyl was synthesized succesfully, and the synthetic technology of its every intermediate was also investigated. The reaction conditions and catalyst were optimized and improved,and the experiment operation was simplified. The yield reached above 90% in each step. The total yield of the product was higher about 20% than the literature value(52.4%), and product purity was over 98.90%.The target compound acibenzolar-S-methyl was synthesized innovatively by benzo[d][1,2,3]thiadiazole-7-carbonyl chloride and sodium methyl mercaptan aqueous solution, whereby avoiding the use of the malodorous and toxic methyl mercaptan and the expensive catalyst DMAP, improving the processing environment, reducing the production cost and achieving a good result.