Imidazo[1,2-a]pyridines are privileged aza-fused heterocyclic scaffolds possessing wide range of applications in medicinal chemistry, organometallics and material science. Imidazo[1,2-a]pyridines functionalized with aroyl group are perceived for their therapeutic applications. However, inaccessibility of this aroylated imidazo[1,2-a]pyridine by Friedel-Crafts reaction had left chemists with an alternate of three-steps long and tiresome protocol as the only source. Hence, in this review we have discussed all the rigorous efforts made in last decade for regioselective and straightforward synthesis of 3-aroyl and 2-aroyl imidazo[1,2-a]pyridines from readily accessible precursors in step-economic pathway. Most importantly, it draws our attention towards the challenge of regioselective aroylation at C-2 position of imidazo[1,2-a]pyridines, as only three methods are reported till date. Graphical Abstract