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Mini-Reviews in Organic Chemistry


ISSN (Print): 1570-193X
ISSN (Online): 1875-6298

Mini-Review Article

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

Author(s): Ramesh Ambatwar, Vaibhav Gupta, Sumit Kumar and Gopal L. Khatik*

Volume 21, Issue 8, 2024

Published on: 07 July, 2023

Page: [811 - 832] Pages: 22

DOI: 10.2174/1570193X20666230601093704

Price: $65


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.

Keywords: Multi-component reaction, Biginelli reaction, dihydropyrimidinones, synthetic methodology, bioactive, heterocyclic scaffolds.

Graphical Abstract
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