Zhou Haixia, He Miao, Liu Chunsheng, Jiang Heng, Luo Genxiang
Department of Chemistry, Liaoning University of Petroleum and Chemical Technology, Fushun, Liaoning, PR China.
Prep Biochem Biotechnol. 2006;36(4):375-81. doi: 10.1080/10826060600912682.
A simple, efficient procedure and improved conditions have been found to carry out the Biginelli reaction for the synthesis of 3,4-dihydropyrimidin-2(1H)-one derivatives. This synthesis was performed using CuBr2 as the catalyst in ethanol solution. The optimum conditions were as follows: the molar ratio of aldehyde to alpha,beta-diketone to urea or thiourea is 1:1:1:0.5, the molar ratio of catalyst to aldehyde is 25%, and the reaction time is 4 h. Under the above conditions, the highest yield of dihydropyrimidinones was up to 95%. Compared with the classical Biginelli reaction conditions, this new method has the advantage of excellent yields and short reaction times.
已发现一种简单、高效的方法及改进的条件来进行用于合成3,4-二氢嘧啶-2(1H)-酮衍生物的Biginelli反应。该合成反应在乙醇溶液中使用CuBr₂作为催化剂进行。最佳条件如下：醛与α,β-二酮与尿素或硫脲的摩尔比为1:1:1:0.5，催化剂与醛的摩尔比为25%，反应时间为4小时。在上述条件下，二氢嘧啶酮的最高产率可达95%。与经典的Biginelli反应条件相比，这种新方法具有产率高和反应时间短的优点。
