1391833-14-9Relevant articles and documents
The use of a lactonized statin side-chain precursor in a concise and efficient assembly of pitavastatin
Fabris, Jan,Casar, Zdenko,Smilovic, Ivanagazi
, 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.