154057-57-5Relevant articles and documents
Preparation method of statins intermediate
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Paragraph 0047-0050, (2018/11/27)
The invention discloses a preparation method of a statins intermediate, comprising the following steps: a phosphate compound and an aldehyde compound are subjected to a condensation reaction under theaction of a catalyst and alkali; after the reaction, post-treatment is conducted to obtain the statins intermediate. The statins intermediate includes a rosuvastatin intermediate (Compound A) and a pitavastatin calcium intermediate (Compound B). The preparation method has the advantages of low cost, simple operation and good yield, is environmentally friendly, and is suitable for industrial production.
The use of a lactonized statin side-chain precursor in a concise and efficient assembly of pitavastatin
Fabris, Jan,Casar, Zdenko,Smilovic, Ivanagazi
experimental part, p. 1700 - 1710 (2012/07/27)
A concise and simple synthetic route to pitavastatin is described. The approach involves a highly stereoselective Wittig olefination reaction between a lactonized statin side-chain precursor and the triphenylphosphonium bromide salt of the corresponding quinoline heterocyclic core. The necessary O-tert-butyl(dimethyl)silyl-protected pitavastatin lactone was obtained in 75% yield and high purity by simple crystallization from aqueous methanol. Subsequent deprotection, hydrolysis, and cation exchange in a one-pot operation provided pitavastatin calcium in 93% yield. Georg Thieme Verlag Stuttgart · New York.