发明名称 |
Omeprazole process and compositions thereof |
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.
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申请公布号 |
US6147103(A) |
申请公布日期 |
2000.11.14 |
申请号 |
US19990387945 |
申请日期 |
1999.09.01 |
申请人 |
MERCK & CO., INC. |
发明人 |
ANOUSIS, NICK;MCMANUS, JAMES W.;BANKS, BENJAMIN NEWTON;ZHOU, LINGWEN |
分类号 |
A61K31/4184;A61P1/04;C07D401/12;(IPC1-7):A61K31/415 |
主分类号 |
A61K31/4184 |
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地址 |
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