Cyanoacetanilide derivatives are important and versatile reagents, which have especially been used for the synthesis of polyfunctionalized five- and six-membered rings and condensed heterocycles. Cyanoacetanilides are poly-functional compounds that possess both electrophilic and nucleophilic properties. The main objective of the present book is to provide a comprehensive account of the synthetic utility of N-aryl and/or heteryl cyanoacetamides in building various organic heterocycles and to highlight their potential in evolving better chemotherapeutic agents.