Year: 2026
Type: preprint
Abstract: A straightforward and green synthetic method has been developed to prepare functionalized 2-arylbenzimidazole derivatives from readily accessible starting materials (arylmethyl alcohols and o-phenylenediamines) via a two-step, one-pot reaction. In the first step, arylmethyl alcohols are oxidized using MnO2 (4-8 equiv.) under both solvent-free and toluene-mediated conditions. subsequently, the aromatic aldehyde undergoes a 10 mol% iodine-catalyzed condensation with o-phenylenediamine in toluene at 100 °C under open-air conditions, leading to the production of 2-substituted benzimidazoles. The one-pot direct conversion of benzyl alcohols to 2-arylbenzimidazoles proceeds efficiently, affording the desired benzofused imidazoles in good to excellent yields, up to 91%. The sustainable method exhibits broad substrate scope, tolerating a wide range of functional groups. Mechanistic studies support a plausible imine formation pathway, followed by cyclization and oxidative aromatization under open-air conditions. This work highlights the synthetic utility and potential of the developed green method for future applications in organic synthesis and medicinal chemistry.
Source: ChemRxiv
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: green
OpenAlex ID: W7213242581