Method for preparing rosuvastatin sodium

US9850213B2 · kind B2 · utility

Assignee

• JIANGXI BOYA SEEHOT PHARMACEUTICAL CO., LTD. · CN

Inventors

• Fener CHEN · Shanghai, CN
• Fangjun XIONG · Shanghai, CN
• Jie Li · Zhejiang, CN
• Pingping Zhan · Shanghai, CN
• Lingjun Xu · Beijing, CN
• Qiuqin HE · Shanghai, CN
• Wenxue CHEN · Tai'an City, CN
• Xiayun Huang · Shanghai, CN
• Yan Wu · Shanghai, CN

Key dates

• Filing date: Jan 10, 2014
• Grant date: Dec 26, 2017
• Expiry date: Feb 13, 2034

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K31/505
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

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…