4-[2-(4,6-二甲氧基嘧啶基)]-3-硫代脲酸苯酯合成工艺及生物活性研究

采用二步反应考察了4-[2-(4,6-二甲氧基嘧啶基)]-3-硫代脲酸苯酯合成的最优反应条件,通过氢谱(1H NMR)、红外光谱(IR)、元素分析和熔点测定,对所合成的产物进行结构分析。采用离体含毒介质法,对合成产物进行杀菌毒力活性的测定。结果表明,0.1 mol氯甲酸苯酯和0.2 mol硫氰酸钾,在乙酸乙酯中50℃反应2 h,滤去生成的氯化钾,加入4,6-二甲氧基嘧啶-2-胺0.08 mol,在60℃下反应4 h,产品总得率不低于75%。产品对植物病害菌有良好的抑制和杀灭作用。

Research on synthesis and biological activity of 4-[ 2-(4,6-D methoxy pyrimidine) ]-3-thiourea carboxylic acid phenoxy ester

The optimal synthesis condition of 4-[2-(4,6-D methoxy pyrimidine)]-3-thiourea carboxylic acid phenoxy ester] were investigated via a two-step reaction.The structure of the product was analyzed by hydrogen spectrum(1H NMR),infrared spectroscopy(IR),element analysis and melting temperature measurement.Meanwhile the bacteria inhibition activity of the product was determined in vitro.The results indicated that the total yield of the product was not less than 75% under the optimal condition:0.1 mol chloroformic acid phenyl ester reacted with 0.2 mol potassium thiocyanate at 50 ℃ for 2 h in the presence of ethyl acetate.Then 0.8 mol 4,6-two methoxy-2-amino pyrimidine was added in and reacted at 60 ℃ for 4 h after removing potassium chloride.The product also exhibited a good inhibition and sterilization to the microorganisms which caused plant diseases.