发明名称 2-4-[4-(4,5-DICHLORO-2-METHYLIMIDAZOLE-1-YL)BUTYL]-1-PIPERAZINYL-5-FLUOROPYRIMIDINE, ITS SYNTHESIS AND THERAPEUTIC USING
摘要 organic chemistry of heterocyclic compounds, medicine, pharmacy. SUBSTANCE: invention relates to a novel 2-4-[4-(4,5-dichloro-2-methylimidazole-1-yl)butyl] -1-piperazinyl-5-fluoropyrimidine of the formula (I) and to its physiologically acceptable salts, for example, citrate, methods of their synthesis and a pharmaceutical composition. The compound of the formula (I) is synthesized by reaction of 8-(5-fluoro-2-pyrimidinyl)-8- aza-5-azoniaspiro-[4,5]-decane with 4-dichloro-2-methyl-1H-imidazole in the presence of potassium carbonate in medium of a polar solvent, for example, dimethylformamide at a boiling point of reaction from 70 C to a solvent boiling point for 3-48 h; or by reaction of 5-fluoro-2-(piperazine-1-yl)-pyrimidine with 1-(4-chlorobutyl-4,5-dichloro- 2-methyl-1H-imidazole under the above indicated conditions or under conditions of the phase transition using an aqueous solution of sodium hydroxide, toluene and a catalyst, for example, tetrabutylammonium bromide at temperature from 50 C to 90 C for from 12 to 72 h. The proposed pharmaceutical composition comprises a compound of the formula (I), its physiologically acceptable salts and a pharmaceutically acceptable base. Compounds of the formula (I) can be used for preparing a medicinal agent designated for treatment of vertigo, transport sick (nausea), depression, troubling state, acid secretion in stomach, obsessive or compulsive disorders, panic attacks and apnea during sleep. EFFECT: new compound indicated above, improved method of synthesis, valuable medicinal properties. 7 cl, 6 ex
申请公布号 RU2191184(C2) 申请公布日期 2002.10.20
申请号 RU20000100371 申请日期 1998.05.28
申请人 LABORATOR'OS DEL' DR. EHSTEV, S.A. 发明人 MERSE-VIDAL' RAMON;FRIGOLA-KONSTANSA KHORDI
分类号 C07D401/12;A61K31/506;A61P1/04;A61P1/08;A61P1/14;A61P11/16;A61P25/08;A61P25/20;A61P25/22;A61P25/24;C07D233/68;C07D239/30;C07D403/12;C07D403/14;(IPC1-7):C07D403/14 主分类号 C07D401/12
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