Background: Coumarin derivatives, characterized by their benzopyrone core, represent a diverse class of natural and synthetic compounds with significant biomedical potential, including antimicrobial, antioxidant, and anticancer activities. Integrating chemical engineering principles into their design, synthesis, and scale-up offers opportunities to optimize production, enhance functionality, and support sustainable biomedical applications. Methods: This review synthesizes literature on the biomedical utilization of coumarin derivatives from a chemical engineering perspective. Emphasis is placed on traditional and green synthetic methodologies, characterization techniques (UV–Vis, FT-IR, NMR, MS, GC), and process optimization strategies. Reaction kinetics, process design, and scale-up approaches are discussed alongside their influence on pharmacological performance. Results: Coumarin derivatives have been effectively synthesized through both classical methods (e.g., Pechmann, Knoevenagel, Perkin reactions) and eco-friendly routes utilizing microwave assistance, solid-supported catalysts, and ionic liquids. Structural characterization confirmed their identity, purity, and functional group modifications. Pharmacological evaluations demonstrated broad biological activity, including potent antimicrobial effects against Gram-positive and Gram-negative bacteria, strong antioxidant properties via free-radical scavenging, and notable anticancer activity through apoptosis induction. The application of chemical engineering principles improved yields, reduced hazardous waste, and facilitated pilot-to-industrial scale transitions while maintaining product quality. Conclusion: The synergy between chemical engineering and medicinal chemistry provides a framework for the sustainable production and biomedical advancement of coumarin derivatives. By aligning synthetic design with reaction kinetics, green chemistry principles, and regulatory safety standards, coumarin-based therapeutics can be developed more efficiently. This interdisciplinary approach holds promise for expanding their role in next-generation drug delivery systems and targeted therapies.
Yasser Fakri Mustafa (Thu,) studied this question.