Benzimidazoles are important components of pharmaceutical compounds owing to their promising bioactivities. The green, safe, and efficient synthesis of benzimidazoles has always been one of the hot topics for chemical workers. α-Chymotrypsin-catalyzed synthesis of benzimidazoles was developed by a reaction between β-keotester and o-phenylenediamine via retro-Claisen reaction. In this eco-friendly medium, a variety of benzimidazole derivatives were obtained in good to excellent yields, with just 10 mg/mL α-Chymotrypsin as catalyst. α-Chymotrypsin catalyzed synthesis of 2-substituted benzimidazole.
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