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Biginelli反应是约120年前意大利化学家Pietro Biginelli发现的,所涉及的就是乙酰乙酸乙酯、尿素和芳基醛的一锅酸催化环化缩合反应.大量的研究表明Biginelli反应的产物——二氢嘧啶酮类化合物因为具有显著的生理和药理活性以及结构变化的多样性使得人们对于Biginelli反应的关注度持续增高.讲述了在微波无溶剂条件下,通过醛、对甲基苯甲酰丙酮、尿素(硫脲)在对甲苯磺酸催化下进行的Biginelli反应的方法来合成5-(4-甲基苯甲酰基)-3,4-二氢嘧啶-2(1H)-酮(硫酮)类衍生物,不仅易得到且收率高.
Biginelli reaction was discovered about 120 years ago by the Italian chemist Pietro Biginelli and involved one-pot acid catalyzed cyclization of ethyl acetoacetate, urea and aryl aldehydes.A large number of studies have shown that the product of the Biginelli reaction, bis Hydropyrimidones have attracted more attentions to the Biginelli reaction because of their remarkable physiological and pharmacological activity and diversity of structures.Recent studies have been made on the reaction of aldehydes, p-methylbenzoylacetone, Synthesis of 5- (4-methylbenzoyl) -3,4-dihydropyrimidin-2 (1H) -one (thione) by the Biginelli reaction of urea (thiourea) catalyzed by p- Derivatives, not only easy to get and high yield.