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In medicinal chemistry, Dihydropyrimidinone-based heterocycle scaffolds have attained a prominent place due to their enormous pharmacological and biological activities. The discovery and development of innovative drugs to combat a wide range of diseases exemplify the utility of these compounds. The present study summarizes the variety of methods available to synthesize various dihydropyrimidinone- based heterocycle scaffolds and their beneficial medicinal properties with the available literature until 2022.