发明名称 Method of preparation of the hemi-calcium salt of (e)-7-[4-(4fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonvl)aminolpyrimidin-5-yl](3r,5s)-3,5-, dihvdroxy-6-heptenoic acid
摘要 A method of preparation of the hemi-calcium salt of rosuvastatin of formula (I) consists in extracting an aqueous solution of the sodium or potassium salt of (E)-7-[4-(4-fluorophenyl)-6isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxy-6-heptenoic acid, with optional admixture of sodium or potassium hydroxide or other sodium or potassium salts having inorganic anions, with an organic solvent, incompletely miscible with water, selected from the series of R<SUP>1</SUP>COOR<SUP>2</SUP>, R<SUP>1</SUP>COR<SUP>2 </SUP>and R<SUP>1</SUP>OH, wherein R<SUP>1 </SUP>and R<SUP>2 </SUP>independently represent hydrogen or a residue of a C<SUB>1</SUB>-C<SUB>10 </SUB>aliphatic hydrocarbon, C<SUB>6 </SUB>aromatic hydrocarbon, C<SUB>5 </SUB>or C<SUB>6</SUB>cyclic hydrocarbon, or a combination of an aliphatic and aromatic or cyclic hydrocarbon, the extract being subsequently shaken with an aqueous solution of an inorganic or C<SUB>1</SUB>-C<SUB>5 </SUB>organic calcium salt, and the product of formula I is further isolated by cooling and/or adding an anti-solvent and filtration, and optionally, is converted into its amorphous form.
申请公布号 US2007155765(A1) 申请公布日期 2007.07.05
申请号 US20040585933 申请日期 2004.12.17
申请人 ZENTIVA, A.S. 发明人 SEBEK PAVEL;RADL STANISLAV;STACH JAN
分类号 A61K31/505;C07D239/42 主分类号 A61K31/505
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