发明名称 HIGH PURITY AMLODIPINE BENZENESULFONATE AND A PROCESS FOR ITS PREPARATION
摘要 3-ethyl 5-methyl (+/-) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5- pyridinedicarboxylate benzenesulfonate, containing overall impurities of significantly less than 0.3% is disclosed, as well as process for its preparation, according to which substance of 3-ethyl 5-methyl (+/-) 2-[2-(N-tritylamino)ethoxymethyl]-4-(2- chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate is converted with benzenesulfonic acid in ethanol solution, at a temperature between 20 DEG C and reflux temperature, followed by isolation and purification of 3-ethyl 5-mehyl (+/-) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4- dihydro-6-methyl-3,5-pyridinedicarboxylate benzenesulfonate. Amlodipine benzenesulfonate is useful as an antiishemic and antihypertensive agent.
申请公布号 WO03004025(A1) 申请公布日期 2003.01.16
申请号 WO2002IB02668 申请日期 2002.07.05
申请人 LEK PHARMACEUTICAL AND CHEMICAL COMPANY D.D.;FURLAN, BORUT;RESNIK, MARIJAN 发明人 FURLAN, BORUT;RESNIK, MARIJAN
分类号 A61K31/4422;A61P9/10;A61P9/12;C07D211/90;(IPC1-7):A61K31/44 主分类号 A61K31/4422
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