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<p>The Biginelli reaction for the synthesis of dihydropyrimidinones was known for more than one century. Due to the biologically and pharmacologically significant of the dihydropyrimidinones, the study of the Biginelli reaction has received constant attention. Additionally, in the view of molecular diversity, the creation of novel multicomponent reactions that yield dihydropyrimidinones has become a major concern in recent years. This review summarizes current developments in the synthesis of dihydropyrimidinones using methods other than the traditional Biginelli reaction, which is based on the interaction of aldehydes and urea/thiourea with other reagents such as acetophenones, alkylaldehydes, 1-substituted acetones, 1-nitroacetones, 1-phosphoryl acetones, dialkyl (trifluoro-2-oxopropyl)phosphonates, 2-oxo-2-polyfluoroalkylethane-1-sulfones, ethanone derivatives, phenyl acetic, enaminones, aroylpropionic acid, α-ketoacid, <i>β</i>-ketophosphonates, cinnamoylacetone, curcumin, oxalacetic acid and its ester, methyl benzoylpyruvate, dialkyl-3-oxoglutarate, diketene, malononitrile, ethyl cyanoacetate, and alkynes. This review serves as a guide for the synthetic methods for the different derivatives of dihydropyrimidinone, where all of the references that were available between 2000 and 2025 were briefly mentioned. </p>

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Synthesis of dihydropyrimidines through strategies beyond the classical Biginelli reaction

  • 期刊论文

  • 发表日期：

    2026年6月24日

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  • Samir Y. Abbas

摘要

The Biginelli reaction for the synthesis of dihydropyrimidinones was known for more than one century. Due to the biologically and pharmacologically significant of the dihydropyrimidinones, the study of the Biginelli reaction has received constant attention. Additionally, in the view of molecular diversity, the creation of novel multicomponent reactions that yield dihydropyrimidinones has become a major concern in recent years. This review summarizes current developments in the synthesis of dihydropyrimidinones using methods other than the traditional Biginelli reaction, which is based on the interaction of aldehydes and urea/thiourea with other reagents such as acetophenones, alkylaldehydes, 1-substituted acetones, 1-nitroacetones, 1-phosphoryl acetones, dialkyl (trifluoro-2-oxopropyl)phosphonates, 2-oxo-2-polyfluoroalkylethane-1-sulfones, ethanone derivatives, phenyl acetic, enaminones, aroylpropionic acid, α-ketoacid, β-ketophosphonates, cinnamoylacetone, curcumin, oxalacetic acid and its ester, methyl benzoylpyruvate, dialkyl-3-oxoglutarate, diketene, malononitrile, ethyl cyanoacetate, and alkynes. This review serves as a guide for the synthetic methods for the different derivatives of dihydropyrimidinone, where all of the references that were available between 2000 and 2025 were briefly mentioned.