Representatives of a new compound family, 9-aryl-5H-imidazo[2,1-d][1,2,5]triazepin-6(7H)-ones have been synthesized. As structural analogues of biologically active 1-aryl-2,3-benzodiazepine-4-ones, these compounds are potential drug candidates in the diseases of the central nervous system. An efficient five-step synthesis starting from imidazole is described here for the preparation of the target compounds. Shorter routes have also been studied, however, these attempts failed.