发明名称 6-BROM-5-HYDROXI-4-DIMETYLAMINOMETYL-1-METYL-2-FENYLTIOMETYLINDOL-3-KARBONSYRA ETYLESTER-HYDROKLORID I MONOHYDRATFORM, FOERFARANDE FOER FRAMSTAELLNING AV DENSAMMA OCH PAA HYDROKLORIDEN I MONOHYDRATFORM BASERAT LAEKEMEDELSPREPARAT MED ANTIVIRUSVERKAN INTERFERONINDUCERANDE OCH IMMUNOMODULERANDE VERKAN
摘要 PCT No. PCT/SU89/00272 Sec. 371 Date Nov. 12, 1991 Sec. 102(e) Date Nov. 12, 1991 PCT Filed Jan. 12, 1989 PCT Pub. No. WO90/08135 PCT Pub. Date Jul. 26, 1990.A novel compound-ethyl 6-bromo-5-hydroxy-4-dimethylaminomethyl-1-methyl-2-phenylthiomethylind ole-3- carboxylate hydrochloride monohydrate having the following formula: <IMAGE> A process for preparing the compound according to the invention, characterized in that it comprises treating ethyl 5-acetoxy-1,2-dimethylindole-3-carboxylate with a brominating agent in an inert organic solvent under reflux, reacting the resultant ethyl 5-acetoxy-6-bromo-2-bromomethyl-1-methylindole-3-carboxylate with thiophenol in the presence of an alkali metal hydroxide or its alcoholate in an organic solvent, reacting the resultant ethyl 6-bromo-5-hydroxy-1-methyl-2-phenylthiomethylindole-3-carboxylate with an aminomethylating agent in an organic solvent at a temperature of from 65 DEG C. to a temperature of refluxing the reaction mixture. The end product is then isolated from the resultant base-ethyl 6-bromo-5-hydroxy-4-dimethylaminomethyl-1-methyl-2-phenylthiomethylind ole-3- carboxylate. The compound according to the invention is an active principle of a pharmaceutical preparation having the antiviral, interferon-inducing and immunomodulatory effects.
申请公布号 SE465462(B) 申请公布日期 1991.09.16
申请号 SE19900000282 申请日期 1990.01.26
申请人 LENINGRADSKY NAUCHNO-ISSLEDOVATELSKY INSTITUT EPIDEMIOLOG;NAUCHNO-ISSLEDOVATELSKY INSTITUT MEDITSINSKOI RADIOLOGII;VSESOJUZNY NAUCHNO-ISSLEDOVATELSKYKHIMIKO-FARMATSEVTICHES 发明人 A N * GRINEV
分类号 A61K31/40;A61K31/403;A61K31/404;A61P31/12;A61P37/00;A61P37/04;A61P43/00;C07D209/42 主分类号 A61K31/40
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