Highly stereoselective formal synthesis of rosuvastatin and pitavastatin through Julia-Kocienski olefination using the lactonized statin side-chain precursor
An expedient and simple synthetic approach to pitava statin and rosuvastatin final intermediates is described. The presented approach consists of completely stereoselective Julia-Kocienski olefination step (E/Z up to 300:1) between lactonized statin side-chain precursor and sulfone derivative of the corresponding pyrimidine and quinoline heterocyclic cores. The desired O-TBS protected statin lactones were isolated in 66-71% yield and high >97% purity (HPLC). Georg Thieme Verlag Stuttgart. New York.
Fabris, Jan,?asar, Zdenko,Smilovi?, Ivana Gazi?,?rnugelj, Martin
p. 2333 - 2346
(2014/12/09)
A PROCESS FOR PREPARATION OF ROSUVASTATIN INTERMEDIATE
The present invention provides an improved process for the preparation of intermediates involved in the preparation of rosuvastatin. Particularly, the proposed invention is able to overcome the disadvantages associated with the known methods. Thus, the instant invention provides a process which is clean, economic, industrially scalable and provides high yields with substantially pure product.
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Page/Page column 17
(2010/04/06)
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