3-Acyloxy-1,4-benzodiazepine-2-ones have found application as hypnosedative anxiolytics. Created in A.V. Bogatsky Physico-Chemical Institute of the NAS of Ukraine and used in medical practice hypnosedative preparation with anxiolytic effect cinazepam (levana® IC) is a representative of this series of compounds. With the aim to search for the nnovel biologically active compounds a series of 3-alkoxy-1,4benzodiazepine-2-ones (1) have been synthesized. It has been established that these compounds show analegesic activity (Fig. 1) and are selective for CBRs of CNS (Fig. 2).               Fig. 1 Analegesic activity.     Fig. 2 Affinity for CBRs of CNS.  The molecular and crystal structures of some representatives of 3-alkoxy-1,4-benzodiazepine-2ones (1) series were established by X-ray analysis. In the crystal cell of 7-bromo-3-cyclopropylmethoxy-5-phenyl-1,2-dihydro-3H-1,4-benzodiazepine-2-one, the formation of dimeric associates due to hydrogen bonds between the amide fragments of adjacent molecules was observed (Fig. 3).