Abstract A facile method for the preparation of N1-(1a–6a) and N3-alkylated (1b–6b) 4- azabenzimidazole derivatives is presented. Both isomers were obtained by alkylation of 4- azabenzimidazole. The isomers were separated, and the preferred formation of the N1- alkylated derivatives (1a–6a) was observed. The C2-proton in the alkylated benzimidazoles can be exchanged for an iodine atom by treatment with methyl lithium and iodine, leading ...