此反应是酸催化的三组分反应，醛，ß-酮酯和脲迅速容易地反应生成二氢嘧啶酮。二氢嘧啶酮是一种非常有用的医药中间体。

反应机理：

机理的第一步通常认为是醛和脲先进行缩合，与 Mannich 缩合有些类似。生成的亚胺离子中间体作为亲电试剂，酮酯烯醇式对其进行亲核加成。生成的中间体的酮羰基与氨基进行缩合得到产品。

最新文献：

N-Substituted Ureas and Thioureas in Biginelli Reaction Promoted by Chlorotrimethylsilane: Convenient Synthesis of N1-Alkyl-, N1-Aryl-, and N1,N3-Dialkyl-3,4-Dihydropyrimidin-2(1H)-(thi)ones
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Organocatalytic Application of Ionic Liquids: [bmim][MeSO4] as a Recyclable Organocatalyst in the Multicomponent Reaction for the Preparation of Dihydropyrimidinones and -thiones
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Ferric chloride/tetraethyl orthosilicate as an efficient system for synthesis of dihydropyrimidinones by Biginelli reaction
I. Cepanec, M. Litvić, A. Bartolinčić, M. Lovrić, Tetrahedron, 2005, 61, 4275-4280.

Ruthenium(III) Chloride-Catalyzed One-Pot Synthesis of 3,4-Dihydro­pyrimidin-2-(1H)-ones under Solvent-Free Conditions
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N-Bromosuccinimide as an Almost Neutral Catalyst for Efficient Synthesis of Dihydropyrimidinones Under Microwave Irradiation
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Catalysis of the Biginelli Reaction by Ferric and Nickel Chloride Hexahydrates. One-Pot Synthesis of 3,4-Dihydropyrimidin-2(1H)-ones
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编译自：Organic Chemistry Portal