A Comparative Review of Conventional and Green Chemistry Approaches of Benzoxaborole Synthesis

Benzoxaboroles are cyclic hemiester versatile scaffolds of boronic acid that demonstrate various pharmacological activities including anti‐fungal, anti‐inflammatory, anti‐malarial, anti‐trypanosomal, anti‐cancer, anti‐pneumococcal and gained significant attention in medicinal chemistry in recent years due to their stable structure. Conventional synthesis methodologies heavily depend on the use of toxic reagents, harsh reaction conditions, harmful by‐products, and higher consumption of energy, which raise environmental issues and economic loss. Green chemistry provides sustainable and efficient routes that use non‐toxic catalysts, eco‐friendly solvents, and less energy‐demanding processes and techniques (catalyst‐free synthesis, green solvents, photocatalysis, microwave‐assisted synthesis, solvent‐free reactions). This review outlines major developments in the green synthesis of benzoxaboroles, providing potential efficient synthetic routes to upgrading conventional practices, thereby contributing to sustainable development goals and their pharmacological importance. While available literature addresses either the conventional or the green synthesis of benzoxaboroles and their derivatives, nonetheless, a notable gap remains regarding reports that combine both methodologies. The current review presents both approaches in a comparative framework. This helps researchers to develop more effective, environmentally friendly synthetic routes and progress in medicinal chemistry.