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Open AccessArticle

Green Synthesis of Privileged Benzimidazole Scaffolds Using Active Deep Eutectic Solvent

1
Dipartimento di Farmacia e Scienze della Salute e della Nutrizione, Dipartimento di Eccellenza L. 232/2016, Edificio Polifunzionale, Università della Calabria, 87036 Rende (CS), Italy
2
Department of Health Sciences, Magna Græcia University, Viale Europa, 88100 Germaneto CZ, Italy
3
ICYTAC, CONICET and Universidad Nacional de Córdoba, Facultad de Ciencias Químicas, Departamento. Química Orgánica. Ciudad Universitaria, Bv. Juan Filloy s/n, 5000 Córdoba, Argentina
4
Dipartimento di Chimica e Tecnologie Chimiche, Via P. Bucci, cubo 12C, Università della Calabria, 87036 Rende (CS), Italy
*
Authors to whom correspondence should be addressed.
Academic Editor: Scott Handy
Molecules 2019, 24(16), 2885; https://doi.org/10.3390/molecules24162885
Received: 9 July 2019 / Revised: 2 August 2019 / Accepted: 7 August 2019 / Published: 8 August 2019
(This article belongs to the Special Issue Deep Eutectic Solvents in Organic Synthesis)
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Abstract

The exploitation and use of alternative synthetic methods, in the face of classical procedures that do not conform to the ethics of green chemistry, represent an ever-present problem in the pharmaceutical industry. The procedures for the synthesis of benzimidazoles have become a focus in synthetic organic chemistry, as they are building blocks of strong interest for the development of compounds with pharmacological activity. Various benzimidazole derivatives exhibit important activities such as antimicrobial, antiviral, anti-inflammatory, and analgesic activities, and some of the already synthesized compounds have found very strong applications in medicine praxis. Here we report a selective and sustainable method for the synthesis of 1,2-disubstituted or 2-substituted benzimidazoles, starting from o-phenylenediamine in the presence of different aldehydes. The use of 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. View Full-Text
Keywords: benzimidazoles; deep eutectic solvents; green chemistry; aromatic amines; heterocyclic moiety benzimidazoles; deep eutectic solvents; green chemistry; aromatic amines; heterocyclic moiety
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Di Gioia, M.L.; Cassano, R.; Costanzo, P.; Herrera Cano, N.; Maiuolo, L.; Nardi, M.; Nicoletta, F.P.; Oliverio, M.; Procopio, A. Green Synthesis of Privileged Benzimidazole Scaffolds Using Active Deep Eutectic Solvent. Molecules 2019, 24, 2885.

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