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The improvement of new synthetic routes towards thiophene, oxazole, triazole, pyrimidine, pyridine, quinolone, coumarin, imidazopyrimidine, pyridoimidazole and triazolo[1,5-a] pyridine for their biological and medicinal exploration is an appealing vicinity for researchers. This review focuses on the utility of 1-(4-substituted-aminophenyl) ethanones and their derivatives as critical intermediates for the synthesis of these systems developed within the closing decade.