FIELD: organic chemistry and technology. SUBSTANCE: product: derivatives of 2-[4-(4-azolylbutyl)-1-piperazinyl] -pyrimidine of the formula (I): where X2 is CR2 where R2 - hydrogen, halogen; X4 is N, CR4 where R4 - hydrogen; X5 is N or R5 where R5 - a lower alkyl; R3 - halogen, or their physiologically acceptable salts. Synthesis of compound (I) is carried out by oxidation of 5-benzyloxy-2-thiomethylpyrimidine to the corresponding sulfone and methylsulfone radical is substituted with piperazine. Synthesized compound is interacted with dibromobutane and formed 8-(5-benzyloxy-2-pyrimidinyl)-8-aza-5-azoniaspiro-[4,5]-decane is condensed with azole of the formula: and obtained compound is deblocked. Pharmaceutical composition has pharmaceutically acceptable vehicle and at least one compound of the formula (I) at amount from 2 to 20 mg. Synthesized compounds are used in medicine since they show anxiolytic or sedative activity. EFFECT: improved method of synthesis. 4 cl, 1 dwg, 4 ex
Authors
Dates
1998-08-27—Published
1994-02-04—Filed