Recently, heterocyclic compounds analogues and their derivatives have attracted strong interest in medicinal chemistry due to their biological and pharmacological properties. The small and simple benzothiazole nucleus possesses numerous biological properties like -antitumor, antimicrobial, anti-inflammatory, anticonvulsant, and antidiabetic activities. These activities are also possessed by its substituted derivatives as well. The present review focuses on some commonly used easy procedures to synthesize the benzothiazole moiety and its derivatives, which comprise of different biological activities.