4-Acetyl-N,N-dialkylbenzenesulfonamides are important and versatile reagents. The main objective of the present book is to provides an overview in the synthesis of 4-acetyl-N,N-dialkylbenzenesulfonamides and used it's as a starting material to synthesized of polyfunctionalized three-, five- and six-membered rings and condensed heterocyclic compounds containing a sulphonamide moiety and to highlight their potential in evolving better chemotherapeutic agents.