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51. 发明申请

WO2010089764A3 IMPROVED PROCESS FOR PREPARATION OF NEBIVOLOL HYDROCHLORIDE 审中-公开
标题翻译：改善NEBIVOLOL HYDROCHLORIDE的制备方法
公开(公告)号：WO2010089764A3
公开(公告)日：2010-11-04
申请号：PCT/IN2010000004
申请日：2010-01-05
申请人： MSN LAB LTD , SATYANARAYANA REDDY MANNE , ESWARAIAH SAJJA , SAHADEVA REDDY MARAMREDDY
发明人： SATYANARAYANA REDDY MANNE , ESWARAIAH SAJJA , SAHADEVA REDDY MARAMREDDY
IPC分类号： C07D311/58 , C07D311/02 , C07D407/00 , C07D407/02 , C07D407/12
CPC分类号： C07D311/58
摘要： An improved process for the preparation of nebivolol and its pharmaceutically acceptable salts is disclosed Concretely, the process involves a) esterifying 6-fluoro-3,4-dihydro-2H-l-benzopyran-2-carboxylic acid to provide alkyl 6-fluoro-3,4-dihydro-2H-l-benzopyran-2-carboxylate, b) reducing the alkyl 6-fluoro-3,4-dihydro-2H-l-benzopyran-2-carboxylate to provide 6-fluoro-3,4-dihydro-2H-l-benzopyran-2-carboxaldehyde, which is subsequently converted to 6-fluoro-3,4-dihydro-2-oxiranyl-2H-l-benzopyran, c) reacting 6-fluoro-3,4-dihydro-2-oxiranyl-2H-l-benzopyran with benzyl amine in a suitable solvent followed by treatment with suitable organic acid, and recrystalhzing the obtained compound to provide the corresponding organic acid salt of benzyl protected nebivolol, d) debenzylating the benzyl protected nebivolol salt, followed by treatment with hydrochloric acid to provide nebivolol hydrochloride
摘要翻译：公开了改进的奈比洛尔及其药学上可接受的盐的制备方法。具体地，该方法包括：a）酯化6-氟-3,4-二氢-2H-1-苯并吡喃-2-羧酸，得到6-氟 - 3,4-二氢-2H-1-苯并吡喃-2-羧酸甲酯，b）还原6-氟-3,4-二氢-2H-1-苯并吡喃-2-羧酸烷基酯，得到6-氟-3,4-二氢-2H- 二氢-2H-1-苯并吡喃-2-甲醛，随后将其转化为6-氟-3,4-二氢-2-环氧乙烷基-2H-1-苯并吡喃，c）使6-氟-3,4-二氢 - 2-环氧乙烷基-2H-1-苯并吡喃与苄基胺在合适的溶剂中随后用合适的有机酸处理，并重结晶所得化合物，得到苄基保护的奈必洛尔的相应有机酸盐，d）使苄基保护的奈比洛尔盐脱苄基化，然后用盐酸处理以提供盐酸奈必洛尔

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