4-苯基-5-乙氧羰基-6-甲基-3,4-二氢嘧啶-2(1H)-酮的绿色合成研究

目的探索操作简便，环境友好的4－苯基－5－乙氧羰基－6－甲基－3，4－二氢嘧啶－2（1H）－酮的合成方法。方法 以苯甲醛、乙酰乙酸乙酯和尿素作为起始原料，在无溶剂和微波加热条件下，选择1－丁基－3－甲基咪唑氯盐和1－丁基－3－甲基咪唑－L－乳酸盐两种不同的离子液体分别催化Biginelli反应制备4－苯基－5－乙氧羰基－6－甲基－3，4－二氢嘧啶－2（1H）－酮，并比较两种离子液体的催化效果。结果两种离子液体在微波、无溶剂条件下均可催化Biginelli反应制得目标化合物，其中1－丁基－3－甲基咪唑－L－乳酸盐作为催化剂目标化合物收率较高。结论以离子液体－丁基－3－甲基眯唑－L－乳酸盐作为催化剂，经微波、无溶剂Biginelli反应制备4－苯基－5－乙氧羰基－6-甲基－3，4－二氢嘧啶－2（1H）－酮，是一种易于操作的绿色合成方法。

Environmentally synthesis of 4-phenyl-5-ethoxycarbonyl-6-methyl-3,4-dihydropirimidine-2(1H)-one

Objective To explore an easily-controled, environmentally benign synthetic method of 4-phenyl-5-ethoxycarbonyl-6-methyl-3,4-dihydropirimidine-2(1H)-one. Methods 4-phenyl-5-ethoxy-carbonyl-6-methyl-3,4-dihydropirimidine-2(1H)-one was synthesized from benzaldehyde, ethyl acetoacetate and urea through the Biginelli reaction catalysed by two different ionic liquid (1-butyl-3-methylimidazolium chloride and 1-butyl-3-methylimidazolium (L)-lactate) under microwave irradiation without a solvent respectively. Results Both ionic liquid catalysts could catalyse Biginelli reaction to get the title compound under microwave irradiation without a solvent. Compared with 1-butyl-3-methylimidazolium chloride, 1-butyl-3-methylimidazolium (L)-lactate was a better catalyst to get a more satisfied yield of the title compound. Conclusion Microwave accelerated solvent-free Biginelli reaction using green ionic liquid of 1-butyl-3-methylimidazolium (L)-lactate as catalyst was a convenient and environmentally benign synthetic method of 4-phenyl-5-ethoxycarbonyl-6-methyl-3,4-dihydropirimidine-2(1H)-one.