Methanol as the C1 source: redox coupling of nitrobenzenes and alcohols for the synthesis of benzimidazoles

We present an operationally simple redox coupling for the synthesis of N-1 substituted benzimidazole using feedstock building block 2-nitroaniline derivatives as the precursors and methanol as the C1 source. Higher atom, step, and redox economy and excellent regioselectivity were achieved compared with the conventional synthesis using diaminobenzene and formic acid derivatives.