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The Highly Efficient Synthesis of 1,2-Disubstituted Benzimidazoles Using Microwave Irradiation
Authors:Monica Nardi  Sonia Bonacci  Natividad Herrera Cano  Manuela Oliverio  Antonio Procopio
Institution:1.Dipartimento di Scienze della Salute, Università Magna Græcia, Viale Europa, Germaneto, 88100 Catanzaro, CZ, Italy; (S.B.); (M.O.); (A.P.);2.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;
Abstract: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.
Keywords:microwave  green chemistry  benzimidazoles  solvent free conditions  Er(OTf)3
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