Among nitrogen‐containing organic compounds, imidazo[1,2‐a]pyridines, and especially C3‐functionalized imidazo[1,2‐a]pyridines, have a wide range of industrial applications in the fields of optics, material science, and organometallics. This scaffolds also have various medicinal uses due to their antiviral, cytotoxic, antibacterial, fungicidal, and antiinflammatory activities as they are found in many commercially available drugs such as Alpidem, Miroprofen, and Zolimidine. In this review, we summarized and classified the latest synthetic methods for the preparation of C3‐functionalized imidazo[1,2‐a]pyridines based on the type of the substituents on the 3‐position of imidazo[1,2‐a]pyridine including C3‐alkylation, C3‐arylation, C3‐carbonylation, C3‐sulfenylation, C3‐selenation, C3‐N‐Substitution, C3‐phosphonation, and C3‐halogenation.
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