Invention Grant
- Patent Title: Method for preparing rosuvastatin sodium
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Application No.: US15038973Application Date: 2014-01-10
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Publication No.: US09850213B2Publication Date: 2017-12-26
- Inventor: Fener Chen , Fangjun Xiong , Jie Li , Pingping Zhan , Lingjun Xu , Qiuqin He , Wenxue Chen , Xiayun Huang , Yan Wu
- Applicant: JiangXi Boya Seehot Pharmaceutical Co., Ltd.
- Applicant Address: CN Fuzhou
- Assignee: JIANGXI BOYA SEEHOT PHARMACEUTICAL CO., LTD.
- Current Assignee: JIANGXI BOYA SEEHOT PHARMACEUTICAL CO., LTD.
- Current Assignee Address: CN Fuzhou
- Agency: Kilpatrick Townsend & Stockton LLP
- Priority: CN201310600552 20131125; CN201310601197 20131125
- International Application: PCT/CN2014/070434 WO 20140110
- International Announcement: WO2015/074328 WO 20150528
- Main IPC: C07D239/42
- IPC: C07D239/42

Abstract:
The present invention belongs to the technical field of organic chemistry, and specifically relates to a method for preparing rosuvastatin sodium. The method of the invention comprises: reducing 4-p-fluorophenyl-6-isopropyl-2-(N-methyl-methylsulfonylamino)pyrimidine-5-carboxylic acid (VII) in the presence of a borohydride, an alkyl-substituted chlorosilane and an assistance in an organic solvent to prepare 4-p-fluorophenyl-5-hydroxymethyl-6-isopropyl-2-(N-methyl-methylsulfonylamino) pyrimidine (VIII); then performing a reaction of the compound VIII with a triphenyl phosphonium salt in an organic solvent to prepare a ((4-p-fluorophenyl-6-isopropyl-2-(N-methyl-methylsulfonylamino)-5-pyridyl)-methyl)triphenyl phosphonium salt (IX); performing a stereoselective Michael addition reaction of (S)-trans-4,5-dihydroxy-pent-2-olefine acid ester (II) with furfural (III) to prepare a 2-((4R,6S)-2-(furan-2-yl)-6-hydroxymethyl-1,3-dioxane-4-yl)acetate (IV); oxidizing the compound IV to prepare a 2-((4R,6S)-2-(furan-2-yl)-6-formacyl-1,3-dioxane-4-yl)acetate (V); performing an olefination reaction of the compound V with the (4-p-fluorophenyl-6-isopropyl-2-(N-methyl-methylsulfonylamino)pyrimid-5-yl)-methyl triphenyl substituted phosphonium salt (IX) or phosphate to prepare 2-((4R,6S)-6-(trans-2-(4-p-fluorophenyl-6-isopropyl-2-(N-methyl-methylsulfonylamino)pyrimid-5-yl)vinyl)-2-(furan-2-yl)-1,3-dioxane-4-yl)acetate (VI); and performing deprotection and sodium salt formation of compound VI to prepare rosuvastatin sodium (I). The method has easily obtainable raw materials, and is simple to operate and suitable for industrial productions.
Public/Granted literature
- US20170183314A1 METHOD FOR PREPARING ROSUVASTATIN SODIUM Public/Granted day:2017-06-29
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