Invention Grant
- Patent Title: Process for preparing pure amorphous rosuvastatin calcuim
- Patent Title (中): 制备纯无定形罗苏伐他汀的方法
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Application No.: US11916599Application Date: 2006-06-22
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Publication No.: US08207333B2Publication Date: 2012-06-26
- Inventor: Zdenko Casar , Marko Zlicar
- Applicant: Zdenko Casar , Marko Zlicar
- Applicant Address: SI Ljubljana
- Assignee: Lek Pharmaceuticals d. d.
- Current Assignee: Lek Pharmaceuticals d. d.
- Current Assignee Address: SI Ljubljana
- Agency: Luedeka Neely Group, P.C.
- Priority: SIP200500187 20050624
- International Application: PCT/EP2006/006008 WO 20060622
- International Announcement: WO2006/136408 WO 20061228
- Main IPC: C07D239/02
- IPC: C07D239/02

Abstract:
A new process for preparing pure amorphous rosuvastatin calcium, substantially free of impurities, is disclosed. A process comprising hydrolysing a C1 to C5 alkyl ester of rosuvastatin, preferably methyl rosuvastatin or tert-butyl rosuvastatin, with a base, e.g. sodium hydroxide, in the presence of an aprotic solvent, preferably tetrahydrofuran and N,N-dimethyl acetamide, or in the presence of a mixture of an aprotic solvent and water, to obtain a solution of rosuvastatin salt, which may be converted to another rosuvastatin salt using another cation, e.g. with calcium cation to obtain rosuvastatin calcium. Rosuvastatin amine salts may be obtained as well.In another preferred aspect of the invention rosuvastatin free acid may be converted to various rosuvastatin salts, e.g. to rosuvastatin calcium, rosuvastatin sodium or various rosuvastatin amine salts, including rosuvastatin solvates, e.g. rosuvastatin calcium hydrate.Rosuvastatin calcium is useful in the treatment of hyperlipidemia, hypercholesterolemia and atherosclerosis.
Public/Granted literature
- US20080188504A1 Process for Preparing Pure Amorphous Rosuvastatin Calcuim Public/Granted day:2008-08-07
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