One important class of organic compounds having many uses, especially in medical chemistry, is benzothiophene and its derivatives. This review examines the biological activity of benzothiophene derivatives and summarizes the synthetic methods used in their production. The effectiveness of several synthetic pathways, such as cyclization techniques, functional group modifications, and reactions catalyzed by transition metals, in gaining access to benzothiophene scaffolds has been examined. Additionally, a broad spectrum of therapeutic domains, such as antiinflammatory, antibacterial, antidiabetic, anticancer, antimicrobial, anti-leishmanial, antifungal, antimalarial, and antitubercular activities, are covered by the pharmacological activities that are being explored. The synthesis and pharmacological potential of benzothiophene derivatives are well-explained in this thorough review, which opens up new options for medicinal chemistry and drug discovery study. Overall, this study is a useful resource for scientists working on drug development and discovery as it sheds light on the pharmacological potential of benzothiophene derivatives. This review includes the synthesis and bioactivities of the years 2002-2024. The goal of this review is to compile the existing information on benzothiophene derivatives and provide guidance for future research and development as well as insights into their possible medicinal uses.