Imidazo[1,2-a]pyrimidine has been receiving significant attention in the synthetic chemistry community through different chemosynthetic methodologies viz., multicomponent reactions, condensation reactions, intramolecular cyclizations, tandem reaction, carbon–hydrogen, carbon–carbon, carbon–nitrogen bond formation, aza-Michael–Mannich reaction, chiral compounds synthesis etc. The mechanisms for the selected reactions are also discussed to observe the formation of this heterocyclic moiety. This review comprehensively summarizes the recently reported various synthetic approaches along with its functionalization at 3-positions to construct this privileged scaffold for further use in the development of new chemosynthetic strategies and drug development due to its wide range of applications in medicinal chemistry.