METHOD OF SYNTHESIS OF HIGH-PURE BUSPYRONE AND ITS HYDROCHLORIDE

FIELD: organic chemistry. SUBSTANCE: product: 8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl] -butyl] -8-aza-spiro- [4.5]decane-7,9-dione (buspyrone) of the formula (I)and its hydrochlorides exhibiting high purity degree. Method of synthesis involves the catalytic hydrogenization of 8-[4-[4-pyrimidine-2-yl)-piperazine-1-yl] -but-2-inyl]-8-aza- spiro[4.5]decane-7,9-dione of the formula (II)in the presence of palladium catalyst or Raney nickel in inert organic solvent and nonobligatory conversion of synthesized thus 8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl-butyl] -8-aza- spiro[4.5] decane-dione to its hydrochloride. Method involves the continuous addition of solution of 8-[4-[4-(pyrimidine-2- yl)-piperazine-1-yl]-but-2-inyl]-8-aza-spiro[4.5]decane-7,9- dione formed by inert organic solvent (at concentration 40 weight%, not less) to the catalyst suspension in inert organic solvent, catalyst removal and, further, a) isolation of the base of 8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl] -butyl] -8- aza-spiro[4.5]decane-7,9-dione, and/or b) treatment of the base of 8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl]-butyl]-8- aza-spiro[4.5] decane-7,9-dione with hydrogen chloride in ethanol or isopropanol at stirring at temperature range from 15 C to 40 C and isolation of 8-[4-[4-(pyrimidine-2-yl)-piperazine-1-yl] -butyl]-8-aza-spiro- [4.5]decane-7,9-dione hydrochloride melting at temperature 188-191 C, or c) treatment of the base of 8-[4-[4-(pyrimidine- 2-yl)-piperazine-1-yl]-butyl]-8-aza-spiro[4.5] decane-7,9-dione with hydrogen chloride in ethyl acetate or isopropanol at temperature 70 C, not above, at stirring and isolation of 8-[4- [4-(pyrimidine-2-yl)-piperazine-1-yl]-butyl]-8-aza-spiro[4.5]- decane-7,9-dione melting at temperature 201-203 C. EFFECT: improved method of synthesis. Настоящее изобретение относится к способу получения 8- [4- [4-(пиримидин-2-ил)-пиперазин-1-ил] -бутил] -8-аза-спиро [4.5]декан-7,9-диона (бус- пирона) формулыи его хлоргидратов, имеющих высокую чистоту, который включает каталитическую гидрогенизацию 8-[4-[4-(пиримидин-2-ил)-пиперазин-1-ил] -бут-2- инил]-8-аза-спиро[4.5]декан-7,9-диона формулыв присутствии палладиевого катализатора или никеля Ренея в инертном органическом растворителе и необязательно превращение полученного таким образом 8- [4- [4-(пиримидин-2-ил)-пиперазин-1-ил] -бутил) -8-аза-спиро[4.5] декан7,9-диона в его хлоргидрат, отличающемуся тем, что осуществляют непрерывное добавление раствора 8-[4-[4-(пиримидин-2-ил)- -пиперазин-1-ил]-