Biginelli Reaction: A Multi-Component Type of Reaction and Synthetic Advancement in the Synthesis of Bioactive Dihydropyrimidinone Derivatives

Background: In synthetic and medicinal chemistry, multi-component reactions (MCRs) are considered an essential tool in synthesizing bioactive heterocyclic scaffolds. These reactions have been strategically used in drug discovery and development because of ease and economy. Objective: The current manuscript aims to highlight the importance of the Biginelli reaction in the synthesis of diverse dihydropyrimidinones with medicinal applications. Methods: We searched various keywords, including “multicomponent reaction”, “Biginelli reaction” and “dihydropyrimidinone” on “PubMed, PubChem, and google scholar” and collected the relevant articles for including the current work. Results: Biginelli reaction involving ketoester, aldehyde, and urea is a high-yielding, atomeconomical, environmentally benign reaction for developing a library of new dihydropyrimidinones to drive the process of drug discovery. Several developments were achieved with modifications of synthetic techniques, including C-H activation, coupling, cycloaddition, etc. Inclusively, these modifications give access to a wide range of dihydropyrimidinones. Conclusion: The current review provides an overview of recent developments in the Biginelli reaction and insights into synthesizing bioactive dihydropyrimidinones.