<p>This review presents thiophene, a compound of major interest due to its increasing importance in medicinal chemistry and materials science. Thiophene is a simple substance playing an essential role in many pharmacokinetic compounds such as antihypertensives, anti-inflammatory drugs, antibacterials, antitumors, anticancers, antituberculosis and antiangiogenics. This study describes the different synthetic methods of thiophene derivatives, such as from a nitrile derivative, a thiol derivative, an amide derivative or a ketone derivative, using different reagents e.g. sulfur, indium chloride, Lawesson's reagent or carbon disulfide, adopting several conditions like reflux, room temperature or microwave, as well as their biological activities.</p> Graphical Abstract <p></p>