Thiophene an important heterocyclic nucleus has been established as the potential scaffold entity in the largely growing chemical world of heterocyclic compounds possessing agrochemical, dyes and potent pharmacological characteristics. The present review, provide a broad view of the synthetic routes of 2-aminothiophenes and further explore their biological profiles and synthetic utility. The knowledge of various synthetic pathways and the diverse physicochemical parameters of 2-aminothiophenes draw the special attention of medicinal chemists to produce combinatorial library and carry out exhaustive efforts in the search of lead molecules.