Sodium Bicarbonate → 4,5-Dimethyl-1H-benzimidazole

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Reaction Steps

3,4-dimethylbenzene-1,2-diamine (300 mg) in 3 mL formic acid was irradiated in a microwave reactor at 150° C. for 5 min. The mixture was diluted with water, neutralized with sat. NaHCO3, then extracted with EtOAc (3×). The organic phase was washed with water and brine, dried (Na2SO4), filtered through a 1″ pad of silica gel and concentrated to afford 320 mg of Intermediate 178.1 as a tan solid. LCMS (2 min gradient) RT=0.90 min, 147.0 (M+H)+.

Provenance & Evidence