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The reaction of 2'-deoxy-5-trimethylsilyl(Tms)uridine with methanesulfonyl chloride led to the corresponding 3',5'-di-O-mesyl derivative, which was treated with lithium toluylate in DMF to give 2,3'-anhydro-1-(2-deoxy-5-O-p-toluyl-beta-D-xylofurano- syl)-5-Tms-uracil. Under these conditions 1-(2,3-dideoxy-5-O-p-toluyl-alpha-D- glycero-pent-2-enofuranosyl)-5-Tms-uracil was obtained from 1-(2-deoxy-alpha-D-ribofuranosyl)-5-Tms-uracil. Interaction of 2,3'-anhydronucleoside with LiN3 in DMF and successive deacylation with MeONa-MeOH gave 3'-azido-2',3'-dideoxy-5-Tms-uridine. Hydrogenation of this compound with 10% Pd/C in ethanol gave 3'-azido-2',3'-dideoxy-5-Tms-uridine. From 2,4,5-tris-Tms-uracil and 2,3-didehydrofurane in 1,2-dichloroethane in the presence of SnCl4 1-(2-tetrahydrofuranyl)-5-Tms-uracil was prepared. In a similar way 1-[(1,3-dioxy-2-propoxy)methyl]-5-Tms-uracil was synthesized by condensation of silylated uracil with 1,3-dibenzyloxy-2-acetoxymethylglycerol followed by the hydrogen transfer hydrogenolysis with cyclohexene--20% Pd(OH)2/C. None of the compounds exhibits cytotoxic activity against CaOv in vitro. The acycloderivative in concentration of 250 micrograms/ml has no effect on the HSV-1 and vaccinia virus replication in vitro. 3'-Azidonucleoside in dose of 100-750 mg/kg as well as 1-(2-tetrahydrofuranyl)-5-Tms-uracil in dose of 160-800 mg/kg were devoid of antitumour activity against P388 in vivo.

It was shown in experiments on mice that the silil derivatives of alpha-pyrrolidone, I-methyl (3-trimethylsilil) pyrrolidone-2 (1A) and 1-vinyl(3 trimethylsilil) pyrrolidone-2 (2A) in doses of 6.25-25 mg/kg exert a tranquilizing effect on emotional behavior of the animals in conflict situation and decrease shock-induced emotional reactions. At the same time IA activates the orienting response and locomotor activity of mice. In the doses that exert the tranquilizing effect the compounds under test increased the content of GABA and speeded up dopamine metabolism in the rat anterior brain. The starting products of the synthesis, 1-methylpyrrolidone-2 and trimethylsilanol given in the test doses produced no tranquilizing effect on the animals' emotional behavior and neuromediator turnover in the brain. It is suggested that the appearance of marked pharmacological activity of the silil derivatives of alpha-pyrrolidone-2 is related to a better penetration of these substances via the hematoencephalic barrier and to their effect on GABA- and dopaminergic processes in the central nervous system.