发明公开
EP0599220A1 A process for the preparation of amlodipine benzenesulphonate
失效
Verfahren zur Herstellung von amlodipin-Benzolsulfonat。
- 专利标题： A process for the preparation of amlodipine benzenesulphonate
- 专利标题（中）： Verfahren zur Herstellung von amlodipin-Benzolsulfonat。
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申请号： EP93118661.3申请日： 1993-11-19
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公开(公告)号： EP0599220A1公开(公告)日： 1994-06-01
- 发明人: Furlan, Borut , Copar, Anton, Dr. , Jeriha, Alenka
- 申请人： LEK, tovarna farmacevtskih in kemicnih izdelkov, d.d.
- 申请人地址： Verovskova 57 SI-61107 Ljubljana SI
- 专利权人： LEK, tovarna farmacevtskih in kemicnih izdelkov, d.d.
- 当前专利权人： LEK, tovarna farmacevtskih in kemicnih izdelkov, d.d.
- 当前专利权人地址： Verovskova 57 SI-61107 Ljubljana SI
- 代理机构： Müller-Boré & Partner Patentanwälte
- 优先权： SI9200344 19921126
- 主分类号： C07D211/90
- IPC分类号： C07D211/90
摘要：
There is disclosed a process for the preparation of 3-ethyl 5-methyl (±) 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridine-dicarboxylate monobenzenesulphonate (amlodipine benzenesulphonate) of formula
wherein 3-ethyl 5-methyl (±) 2-[2-(N-tritylamino)-ethoxymethyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate is reacted with benzenesulphonic acid in a methanolic or an aqueous methanolic medium at a temperature from 20 °C to the reflux temperature and the title compound is isolated and purified.
Amlodipine benzene sulphonate is a valuable anti-ischaemic and anti-hypertensive agent.
wherein 3-ethyl 5-methyl (±) 2-[2-(N-tritylamino)-ethoxymethyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylate is reacted with benzenesulphonic acid in a methanolic or an aqueous methanolic medium at a temperature from 20 °C to the reflux temperature and the title compound is isolated and purified.
Amlodipine benzene sulphonate is a valuable anti-ischaemic and anti-hypertensive agent.
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