Benzoxazepine is a bi-cyclic heterocyclic compound of a benzene ring fused to an oxazepine ring. Various benzoxazepine derivatives have been synthesized and evaluated for various biological activities. Some analogs derivatives have shown potent biological activities and may be considered as lead molecule for the development of future drugs. This review highlights the different biological activities like anticonvulsant, antimicrobial, anticancer, antipsychotic agents, calcium antagonists and neuroprotective. Since no comprehensive review on biological potential of benxozapine is available, this review covers all the literature reports with patents by giving emphasis on synthetic schemes and biological activities of the different benzoxazepine analogs.