Exceedingly facile single-step expedient protocols based on the versatility and reactivity of corresponding intermediates amidine and imidate (8 and 9), derived from 5-carboxamido-1,4-benzodiazepin-5-(4'-methylpiperazinyl)-carboxamide have been developed to provide an easy installation of the oxadiazole, pyrimidine, imidazole and benzimidazole (9-14) based privileged templates at 2-position of 5-carboxamido-1,4-benzodiazepin-5-(4'-methylpiperazinyl)-carboxamide (4), through a phenoxyl spacer, by utilizing the synthetic strategy depicted in schemes 1 and 2.