期刊
SYNTHESIS-STUTTGART
卷 44, 期 11, 页码 1700-1710出版社
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0031-1290916
关键词
Wittig reactions; heterocycles; quinolines; lactones; drugs
资金
- Lek Pharmaceuticals d.d.
- EN-FIST Centre of Excellence
- Public Agency for Technology of the Republic of Slovenia (TIA) [MR-10/75]
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.
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