The present endeavor embodies studies pertaining to the development of nitrogen containing fused ring systems as potential central nervous system active agents. The thesis has been organized into three sections, each section includes five chapters. The studies cover all the aspects of medicinal chemistry research, starting from synthetic organic chemistry to biological activity and eventually the molecular docking of active compounds. Few privileged scaffolds have been identified for the current study. One of them is 3-benzazepine, a seven membered bicyclic benzoannelated fused ring system. Several protocols have been reported in literature for the cyclization and substitution on 3-benzazepine scaffold. As focus of the study was to synthesize C-1 substituted 3-benzazepin-2-one scaffold, a direct arylation method was tried with the help of palladium chemistry.