The synthesis and investigation of psychotropic activity of some derivatives of 4-(2-oxopropylidene)-1,5- benzodiazepine-2-one are reported. The alkylation reactions were conducted under the conditions of phase transfer catalysis. Interestingly, the acute toxicity according to the European protocol in two mammal species appropriate to assess the lethal doses was evaluated. In addition, we studied the effects of these products on the central nervous system through a battery of behavioral tests used in psychopharmacology. The results obtained show a lack of toxicity at therapeutic doses. The products exert sedative effects at different degrees with respect to the same reference, clobazam, and lengthen the hypnotic effect of Tranxene