Invention Grant
US08049010B2 Synthetic method and intermediates of Rosuvastatin calcium and preparation methods of intermediates
有权
罗苏伐他汀钙的合成方法和中间体及其中间体的制备方法
- Patent Title: Synthetic method and intermediates of Rosuvastatin calcium and preparation methods of intermediates
- Patent Title (中): 罗苏伐他汀钙的合成方法和中间体及其中间体的制备方法
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Application No.: US11795123Application Date: 2005-11-18
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Publication No.: US08049010B2Publication Date: 2011-11-01
- Inventor: Qingyun Huang
- Applicant: Qingyun Huang
- Applicant Address: CN Anhui
- Assignee: Anhui Qingyun Pharmaceuticals & Chemical Co., Ltd.
- Current Assignee: Anhui Qingyun Pharmaceuticals & Chemical Co., Ltd.
- Current Assignee Address: CN Anhui
- Agency: Ostrow Kaufman LLP
- Agent Antonio Papageorgiou
- Priority: CN200510038203 20050119
- International Application: PCT/CN2005/001958 WO 20051118
- International Announcement: WO2006/076845 WO 20060727
- Main IPC: C07D239/42
- IPC: C07D239/42 ; C07D405/06 ; C07D403/12 ; C07D413/12

Abstract:
The present invention publicly discloses a synthetic method and intermediates of rosuvastatin calcium and synthetic methods of the intermediates. The synthetic method uses 4-4′-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyridine-5-formaldehyde as the raw material, includes 4-4′-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyridine-5-acrylonitrile (intermediate I) from a nitrilized reaction, and 4-4′-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyridine-5-acraldehyde (intermediate II) from an aldehydized reaction of the intermediate I, and further goes through such unit processes as side-chain extension, ketone-group reduction, ethyl-group hydrolysis and neutralization reaction or decomposition reaction to obtain rosuvastatin calcium. The nitrilized reagent can be phosphate diethylacetonitrile, acetonitrile, etc.; the aldehyde reductant can be diisobutyl aluminum hydride, red aluminum, etc.; and the ketone-group reductant can be diethylmethoxyborane, NaBH4, KBH4, etc.
Public/Granted literature
- US20080091014A1 Synthetic Method and Intermediates of Rosuvastatin Calcium and Preparation Methods of Intermediates Public/Granted day:2008-04-17
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