Journal Article

Green Synthesis of Privileged Benzimidazole Scaffolds Using Active Deep Eutectic Solvent

Procopio, Antonio, Di Gioia, Maria Luisa, Nardi, Monica, Cassano, Roberta, Maiuolo, Loredana, Costanzo, Paola, Oliverio, Manuela, Nicoletta, Fiore Pasquale, Herrera Cano, Natividad

2019

Overview

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 -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.

• Publisher: MDPI AG,MDPI
• Subject: Aldehydes / Analgesics / Antiinfectives and antibacterials / aromatic amines / Benzimidazoles / Benzimidazoles - chemical synthesis / Benzimidazoles - chemistry / Chemistry / Chloride / Chromatography / deep eutectic solvents / Environmental impact / Green chemistry / Green Chemistry Technology / heterocyclic moiety / Hydrogen bonds / Inflammation / Molecular Structure / Organic chemistry / Pharmaceutical industry / Phenylenediamine / Reagents / Solvents / Solvents - chemistry / Spectrum Analysis