二氢嘧啶类药物活性化合物的绿色合成研究.doc

二氢卩密睫类药物活性化合物的绿色合成研究（三） 摘要 二氢囉噪衍牛物在医学领域的应用广泛，因此人们越来越重视二氢嗨噪衍牛物的合 成。离子液体因其具有独特的绿色催化、高活性和热稳定性好等特点而符合绿色化学的耍 求。杂多酸类离子液体屮的无机阴离子是由杂多酸构成的，杂多酸离子液体在一些氧化、 脱水和缩合反应屮都表现出优良的催化活性和易回收循环的性质，而此次实验研究则充分 利用了杂多酸离子液体的绿色催化性能。以苯甲醛、乙酰乙酸乙酯、尿素为反应模型，对 离子液体催化剂的催化性能进行筛选，催化剂[PS-Py]3PW12O40产率最高。针对催化活性最 高的催化剂进行反应条件优化，得出最优化的实验条件。最优化的反应条件为：苯甲醛、 乙酰乙酸乙酯、尿素和催化剂的投料摩尔比为1:1.5:1.5:0.03,反应温^ 120-130°Co以优化 的实验条件对反应进行扩展，通过改变不同的底物，对反应适用范围进行探索，产率能达 到89%?94%。对Biginelli反应的绿色合成进行研究，实现了二氢“密呢类化合物的无溶剂绿 色合成，为二氢“密噪类化合物的合成提供了绿色合成新途径。 关键词：二氢喀唳绿色化学杂多酸离子液体 Green Synthesis of dihydropyrimidine drugs active compounds(HI) Abstract Dihydropyrimidine derivatives are widely used in the medical field, so there is a growing emphasis on the syn thesis of dihydropyridi ne derivatives .Ionic liquids meets the requireme nts of green chemistry because of its unique green catalysis, high activity, thermal stability and other good features..!norganic anions in heteropoly acids ionic liquids are composed of heteropolyacids.Heteropoly acid ionic liquids exhibited some properties such as,excellent catalytic activity and ease of recovery and recycling in some oxidation, dehydration and conde nsati on react io n. And this experimental study make full use of green catalytic performa nee of ionic liquids heteropolyacid .Benzaldehyde, ethyl acetoacetate, urea as the reaction model, the catalytic performanee of the ionic liquid catalyst is filtered, and the catalyst [PS-Py]3PWi204o has the highest yield.Experimental conditions were optimized for the highest activity of the catalyst,and then we can drawn optimized experimental conditions. Optimized reaction conditions: benzaldehyde ethylacetoacetate、 urea and catalyst molar ratio 1:1.5:1.5:0.03 feeding,the reaction temperature 120?13CTC?By changing the type of substrate, to explore the scope of the reaction, the yield can reach 89%-94%.Doing research on green synthesis of Biginelli reaction to achieve the green synthesis of dihydropyrimidine compounds without solve nt. And it provides a new way of