Abstract
A methodology is reported for the preparation of 2-aryl-benzimidazole-3-oxide derivatives. By means of a one-pot two-step protocol, a library of 42 new compounds has been prepared. Reactions were performed in a total time of 40 min using microwave heating as a tool. A streamlined work-up process was also developed, allowing for facile isolation of the products. The methodology offers a more sustainable approach than previous routes, with only water and ethanol being used as solvents, and the products being isolated by means of a simple filtration without the need for any further purification.
Highlights
Nitrogen-containing heterocyclic compounds play a vital role in drug development because they can increase binding efficiency and solubility as well as facilitate the formation of salts
The benzimidazole scaffold falls into this category
This motif is present in several commercial available pharmaceuticals that are used for the treatment of different diseases and disorders, such as ulcers, high blood pressure, tumors, and allergies, as well as fungal, bacterial, and viral infections (Figure 1) [3,4,5,6]
Summary
Nitrogen-containing heterocyclic compounds play a vital role in drug development because they can increase binding efficiency and solubility as well as facilitate the formation of salts. These properties improve oral absorption and bioavailability of the drug [1,2]. The benzimidazole scaffold falls into this category. This motif is present in several commercial available pharmaceuticals that are used for the treatment of different diseases and disorders, such as ulcers, high blood pressure, tumors, and allergies, as well as fungal, bacterial, and viral infections (Figure 1) [3,4,5,6]. The wide range of applications of benzimidazole derivatives has reignited interest in the development of improved synthetic routes
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