Heterocycles are the main structural motif of DNA and RNA and play a crucial role in various
chemical reactions of metabolisms. Therefore, heterocyclic compounds show good physiological and pharmacological
properties. Coumarin and pyrazole scaffolds are present in many commercial drug molecules and
natural products. This review overviews the progress made in the synthesis and functionalization of the coumarin-
pyrazole hybrid heterocycle. It also includes discussion on the possible reactive sites of heterocycles,
functionalization, and mechanistic pathways to incorporate pyrazole pharmacophore unit in synthesis. Several
synthesis and biological studies reveal that the combination of the coumarin-pyrazole moiety is a prominent
structural motif to find lead compounds in drug discovery.
Keywords: Coumarin-pyrazole, Vilsmeier-Haack, formylation, multicomponent reactions, heterocycles, DNA.
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