2,3-Diaminotoluene → 4-Methylbenzimidazole

Participants

Reaction Steps

A solution of 3-methylbenzene-1,2-diamine (170 mg) in formic acid (2 mL) was heated at 140° C. for 5 min in a microwave reactor. The mixture was diluted with water, neutralized with sat. NaHCO3, then extracted with EtOAc. The organic phase was washed with water and brine, dried (Na2SO4), filtered through a 1″ pad of silica gel and concentrated to afford 122 mg of Intermediate 171.1 as a tan solid.

Provenance & Evidence