Benzimidazole is one of the heterocycles associated with diverse biological potential such as anthelmintic, antacid, antimicrobial, anticancer, and antiviral. Based on the importance of this moiety in medicinal drugs, both clinically approved and in clinical trials, many novel synthetic approaches have been reported for benzimidazoles. Nonetheless, there is a need for novel benzimidazoles to overcome drug resistance and side effects. The present review covers the recent reports on benzimidazole synthesis using a different strategy, our work on the synthesis, and biologically potent novel benzimidazoles.