四氢嘧啶类化合物的合成

以羰基衍生物，取代1,3-二羰基化合物，脲和硫脲为原料，经固定化青霉素酰化酶催化的Biginelli反应合成了22个四氢嘧啶类化合物（1a~1v），其中1s和1v为新化合物，其结构经¹H NMR， ¹³C NHR和IR表征。研究了溶剂、反应温度、反应时间和物料比γ［n(苯甲醛) ：n(脲) ：n(乙酰乙酸乙酯)］对1a产率的影响。结果表明：在最佳反应条件（固定化青霉素酰化酶为催化剂，乙醇为溶剂，γ=1.0 ：1.5：1.0，于50 ℃反应6 h）下，1a产率最高（85%）。

Syntheses of Tetrahydro-pyrimidine Compounds

Twenty-two tetrahydro-pyrimidines(1a～1v, 1s and 1v were novel compounds) were synthesized using carbonyl derivatives, substituted 1,3-dicarbonyl compounds, urea and thiourea as the starting materials, by an efficient immobilized penicillin G amidase catalyzed Biginelli reaction.The structures were characterized by 1H NMR , 13C NHR and IR.The effects of solvent, reaction temperature, reaction time and materials ratio γn(benzaldehyde)∶n(urea)∶n(ethyl acetoacetate)] on the yield of 1a were researched.The results showed that 1a could be obtained with the highest yield (85%) under the optimum reaction conditions (immobilized penicillin G amidase as the catalyst, ethanol as the solvent, γ=1.0 ∶1.5 ∶1.0, at 50 ℃ for 6 h).