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A mild, one-pot synthesis of disubstituted benzimidazoles from 2-nitroanilines
Authors:Keith R Hornberger  George M Adjabeng  Hamilton D Dickson  Ronda G Davis-Ward
Institution:Department of Chemistry, Microbial, Musculoskeletal, and Proliferative Diseases Center of Excellence for Drug Discovery, GlaxoSmithKline, Research Triangle Park, NC 27709, USA
Abstract:A one-pot synthesis of disubstituted benzimidazoles from 2-nitroanilines is described. Hydrogenation of N-substituted 2-nitroanilines with palladium on carbon as catalyst in the presence of trimethyl orthoformate and catalytic pyridinium p-toluenesulfonate (PPTS) at room temperature provided good to excellent yields of the corresponding disubstituted benzimidazoles.
Keywords:Benzimidazoles  Hydrogenation  Cyclocondensation
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