N-甲基嘧啶酮类化合物的绿色合成研究

Research on Green Synthesis of N-Methylpyrimidine Ketone Compounds

经典的Biginelli反应有其操作简单易于实现的优势,同时也有一定的不足,比如其反应耗时较长,得到的目标产物较少产率低,性价比,而且使用的浓盐酸来作为反应催化剂,会对设备造成严重腐蚀,并且污染环境。所以我们要更换催化剂来优化反应条件,从而达到减小污染,减少试验时间的目的。在本篇文章中,通过将各种甲基脲和β-酮酸酯(包括乙酯,异丙酯,苯甲酰乙酸乙酯等)作为原材料,合成了N-甲基嘧啶酮类化合物,完成了此反应的绿色合成研究。

The process of classical Biginelli reaction is easy to operate, however the yield is low with only 20% - 50% and has a long reactiontime; Besides, the corrosion resistance of concentrated hydrochloric acid catalyst on reaction equipment is strong and it will bring damage to theenvironment. So finding suitable catalyst and accelerant, shortening the reaction time and optimizing the reaction conditions become the researchhot topics in recent years. In this paper, with the aromatic aldehyde, and methyl urea, β-keto ester (including methyl acetoacetate, ethyl ester, propylacetate, isopropyl acetate, n-butyl acetate, ethyl benzoyl acetate) as raw materials, make the synthesis of six series of N - methyl replacing 3, 4 dihydropyrimidine - 2 - ketone and get the green synthesis of chemical reaction.