The presence of benzoxazole moiety in most of the heterocyclic compounds is well reported. The present literature review mainly highlights the novel synthetic transformation and describes the biological potential of most of the heterocyclic compounds by virtue of presence of benzoxazole framework. Most of the researchers have revealed that benzoxazole derivatives exhibit significant antibacterial, anti-inflammatory, antifungal, anticancer, analgesic, antiviral, anti-tubercular, and anthelmintic activities. Benzoxazole moieties also act as tyrosinase inhibitor and cholesterol ester transfer protein inhibitor. This literature review may provide an opportunity to the chemists to design new derivatives of benzoxazole that proved to be the successful agent in view of safety, effectiveness, and efficacy.