Green Synthesis of Privileged Benzimidazole Scaolds Using Active Deep Eutectic Solvent

DI GIOIA MARIA LUISA; CASSANO, ROBERTA; COSTANZO, PAOLA; HERRERA CANO, NATIVIDAD; MAIUOLO, LOREDANA; NARDI MONICA; NICOLETTA, FIORE PASQUALE; OLIVERIO MANUELA; PROCOPIO, ANTONIO

MOLECULES

MOLECULAR DIVERSITY PRESERVATION INTERNATIONAL-MDPI

Lugar: Basel; Año: 2019

1420-3049

The exploitation and use of alternative synthetic methods, in the face of classical proceduresthat do not conform to the ethics of green chemistry, represent an ever-present problem in thepharmaceutical industry. The procedures for the synthesis of benzimidazoles have become a focusin synthetic organic chemistry, as they are building blocks of strong interest for the developmentof compounds with pharmacological activity. Various benzimidazole derivatives exhibit importantactivities such as antimicrobial, antiviral, anti-inflammatory, and analgesic activities, and some ofthe already synthesized compounds have found very strong applications in medicine praxis. Herewe report a selective and sustainable method for the synthesis of 1,2-disubstituted or 2-substitutedbenzimidazoles, starting from o-phenylenediamine in the presence of dierent aldehydes. The useof deep eutectic solvent (DES), both as reaction medium and reagent without any external solvent,provides advantages in terms of yields as well as in the work up procedure of the reaction.