A solid-phase synthetic route to substituted 7-azabenzimidazoles suitable for combinatorial library synthesis

A novel route for the solid-phase synthesis of 1,2,5-substituted 7-azabenzimidazole derivatives has been developed. Primary amines are attached to an aldehyde resin then coupled to 6-chloro-5-nitro-nicotinyl chloride. Subsequent alkylation with amines, reduction of the nitro group and cyclisation with aldehydes gives 1,2,5-substituted 7-azabenzimidazole derivatives.