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1. 发明授权

US06191148B1 Omerazole process and compositions thereof 有权
标题翻译：奥美拉唑法及其组合物
公开(公告)号：US06191148B1
公开(公告)日：2001-02-20
申请号：US09461605
申请日：1999-12-15
申请人： James W. McManus , Nick Anousis , Benjamin Newton Banks , Hui Liu , Lingwen Zhou
发明人： James W. McManus , Nick Anousis , Benjamin Newton Banks , Hui Liu , Lingwen Zhou
IPC分类号： A61K314439
CPC分类号： C07D401/12
摘要： The present invention describes an improved process for the preparation, isolation, and purification of the anti-ulcer agent omeprazole whereby the sulfide precursor pyrmetazole is reacted subsurfacely with exactly one molar equivalent of meta-chloroperoxybenzoic acid in a chlorinated aliphatic hydrocarbon or aromatic hydrocarbon solvent, such as methylene chloride or toluene; residual organic solvent is removed from the aqueous layer by vacuum distillation; crude product is obtained by reactive crystallization with an alkyl formate or formic acid solution and seeding; and pure product is isolated by recrystallization in methanol-water containing aqueous NaOH by subsurface addition of aqueous acetic acid to pH 9.0, seeding, filtration, washing, and drying. Omeprazole and compositions of omeprazole containing no chromatographically detectable levels of residual non-alcoholic organic reaction solvent and diminished levels of alcoholic solvent are also described.
摘要翻译：本发明描述了一种用于制备，分离和纯化抗溃疡剂奥美拉唑的改进方法，其中硫化物前体pyrmetazole在氯代脂族烃或芳族烃溶剂中与恰好一摩尔当量的间氯过氧苯甲酸在地下反应，如二氯甲烷或甲苯; 通过真空蒸馏从水层除去残留的有机溶剂; 粗产物通过与甲酸烷基酯或甲酸溶液反应结晶并接种获得; 通过在甲醇 - 含水NaOH水溶液中再次析出纯产物，通过地下加入乙酸水溶液至pH 9.0，接种，过滤，洗涤和干燥。还描述了奥美拉唑和不含色谱可检测水平的残留的非酒精有机反应溶剂和降低的醇溶剂水平的奥美拉唑组合物。

2. 发明授权

US6147103A Omeprazole process and compositions thereof 有权
公开(公告)号：US6147103A
公开(公告)日：2000-11-14
申请号：US387945
申请日：1999-09-01
申请人： Nick Anousis , James W. McManus , Benjamin Newton Banks , Lingwen Zhou
发明人： Nick Anousis , James W. McManus , Benjamin Newton Banks , Lingwen Zhou
IPC分类号： A61K31/4184 , A61P1/04 , C07D401/12 , A61K31/415
CPC分类号： C07D401/12
摘要： The present invention describes an improved process for the preparation, isolation, and purification of the anti-ulcer agent omeprazole whereby the sulfide precursor pyrmetazole is reacted subsurfacely with exactly one molar equivalent of meta-chloroperoxybenzoic acid in methylene chloride or toluene solution; residual organic solvent is removed from the aqueous layer by vacuum distillation; crude product is obtained by reactive crystallization with an alkyl formate and seeding; and pure product is isolated by recrystallization in methanol-water containing aqueous NaOH by subsurface addition of aqueous acetic acid to pH 9.0, seeding, filtration, washing, and drying. Compositions of omeprazole containing no chromatographically detectable levels of residual non-alcoholic organic reaction solvent are also described.

3. 发明授权

US6166213A Omeprazole process and compositions thereof 有权
标题翻译：奥美拉唑方法及其组合物
公开(公告)号：US6166213A
公开(公告)日：2000-12-26
申请号：US169231
申请日：1998-10-09
申请人： Nick Anousis , James W. McManus , Benjamin Newton Banks , Lingwen Zhou , Hui Liu
发明人： Nick Anousis , James W. McManus , Benjamin Newton Banks , Lingwen Zhou , Hui Liu
IPC分类号： A61K31/4184 , A61P1/04 , C07D401/12
CPC分类号： C07D401/12
摘要： The present invention describes an improved process for the preparation, isolation, and purification of the anti-ulcer agent omeprazole whereby the sulfide precursor pyrmetazole is reacted subsurfacely with exactly one molar equivalent of meta-chloroperoxybenzoic acid in methylene chloride or toluene solution; residual organic solvent is removed from the aqueous layer by vacuum distillation; crude product is obtained by reactive crystallization with an alkyl formate and seeding; and pure product is isolated by recrystallization in methanol-water containing aqueous NaOH by subsurface addition of aqueous acetic acid to pH 9.0, seeding, filtration, washing, and drying. Compositions of omeprazole containing no chromatographically detectable levels of residual non-alcoholic organic reaction solvent are also described.
摘要翻译：本发明描述了一种用于制备，分离和纯化抗溃疡剂奥美拉唑的改进方法，其中硫化物前体吡咪唑与正好一摩尔当量的间氯过氧苯甲酸在二氯甲烷或甲苯溶液中地下反应; 通过真空蒸馏从水层除去残留的有机溶剂; 粗产物通过与甲酸烷基酯反应结晶并接种获得; 通过在甲醇 - 含水NaOH水溶液中再次析出纯产物，通过地下加入乙酸水溶液至pH 9.0，接种，过滤，洗涤和干燥。还描述了不含色谱可检测水平的残留非醇有机反应溶剂的奥美拉唑组合物。

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