The Highly Efficient Synthesis of 1,2-Disubstituted Benzimidazoles Using Microwave Irradiation

oleh: Monica Nardi, Sonia Bonacci, Natividad Herrera Cano, Manuela Oliverio, Antonio Procopio

Format: Article
Diterbitkan: MDPI AG 2022-03-01

Deskripsi

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 <i>N</i>-phenyl-<i>o</i>-phenylenediamine:benzaldehyde (1:1) using microwave irradiation and only 1% mol of Er(OTf)<sub>3</sub> 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.