Considering the essential biological and medicinal properties of chalcones, the synthesis of these compounds has attracted the interest of medicinal and organic chemists. This review aims to describe the different strategies developed so far for the synthesis of chalcones and their applications. After a brief introduction of the chalcones and their biological activities, different synthetic approaches such as chemical and other methods are described and organized on the basis of the catalysts and the other reagents employed in the syntheses. Some of the reactions have been applied successfully to the synthesis of biologically important compounds. Moreover, the biological and pharmacological activities of chalcones have been shown.