Sultams are very important scaffolds both in medicinal chemistry and in synthetic organic chemistry. Very important methodologies for the asymmetric and non‐asymmetric synthesis of sultams, including asymmetric synthesis with memory of chirality (MOC), have recently been developed. Nowadays sultams are tremendously widely applied both in the medicinal field and in the synthetic field for the synthesis of different natural and non‐natural heterocycles. This review covers the recent development (2011–June 2017) of powerful methodologies for the synthesis of sultams and their applications in various fields during this period. A critical view of the mechanisms of the developed methodologies together with the scope and limitations of these methods add an extra dimension to the text.

A one-pot method for the Sonogashira coupling and cyclization of 2-bromobenzenesulfonamides and terminal alkynes is presented. This method allows access to a variety of substituted benzosultams regioselectively in excellent yields. The reasons for regioselectivity are interpreted through density functional theory (DFT) studies.

A new series of 2‐aminodiarylsulfones have been prepared from N‐alkyl‐N‐arylbenzenesulfonamides by Fries‐type rearrangement. Some aspects like regioselectivity, high yields and short reaction times make this rearrangement much more attractive. The structures of the 2‐aminodiarylsulfones are confirmed from single crystal XRD analysis.

An efficient method for the regioselective synthesis of uracil-, coumarin-and quinolone-fused benzosultams and benzosultones is reported. The method offers a synthetic route to highly functionalized sultam and sultone derivatives in 75-95% yield under mild conditions. Density functional theory studies have been used to explain the regioselectivity in the synthesis of the coumarin-and quinolone-fused sultams and sultones.

Synthesis of a series of five-membered sultams containing different hetero-or carbocycles were obtained in good to excellent yields by ring-closing metathesis (RCM) reaction. Many sultams were precipitated from the reaction mixture and they were easily separated by filtration without further purification.