The Highly Efficient Synthesis of 1,2-Disubstituted Benzimidazoles Using Microwave Irradiation
Monica Nardi,
Sonia Bonacci,
Natividad Herrera Cano,
Manuela Oliverio,
Antonio Procopio
Affiliations
Monica Nardi
Dipartimento di Scienze della Salute, Università Magna Græcia, Viale Europa, Germaneto, 88100 Catanzaro, CZ, Italy
Sonia Bonacci
Dipartimento di Scienze della Salute, Università Magna Græcia, Viale Europa, Germaneto, 88100 Catanzaro, CZ, Italy
Natividad Herrera Cano
ICYTAC, Instituto de Ciencia y Tecnología de Alimentos de Córdoba, CONICET, Departamento de Química Orgánica, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, Bv. Juan Filloy s/n, Córdoba 5000, Argentina
Manuela Oliverio
Dipartimento di Scienze della Salute, Università Magna Græcia, Viale Europa, Germaneto, 88100 Catanzaro, CZ, Italy
Antonio Procopio
Dipartimento di Scienze della Salute, Università Magna Græcia, Viale Europa, Germaneto, 88100 Catanzaro, CZ, Italy
The benzimidazole ring of the heterocyclic pharmacophores is one of the most widespread and studied systems in nature. The benzimidazole derivative synthesis study is a crucial point for the development of a clinically available benzimidazole-based drug. Here, we report a simple microwave assisted method for the synthesis of 1,2-disubstituted benzimidazoles. The combination of the molar ratio of N-phenyl-o-phenylenediamine:benzaldehyde (1:1) using microwave irradiation and only 1% mol of Er(OTf)3 provides an efficient and environmental mild access to a diversity of benzimidazoles under solvent-free conditions. The proposed method allows for the obtainment of the desired products in a short time and with very high selectivity.
