<p>Atorvastatin lactone is prepared by hydrogenating tert-butyl isopropylidene nitrile to tert-butyl isopropylidene amine and condensing the amine with the diketone of atorvastatin to form acetonide ester. The diol protecting acetonide ester is deprotected to form a diol ester by dissolving the acetonide ester in methanol and treating with an acid. The diol ester is saponified to form a sodium salt. Methanol is removed from the reaction mixture by distillation. The sodium salt is reacidified to the free diol acid and atorvastatin lactone is formed from the diol acid. The atorvastatin lactone is directly dried without further purification.</p>
申请公布号
WO2007029216(A1)
申请公布日期
2007.03.15
申请号
WO2005IE00094
申请日期
2005.09.09
申请人
PFIZER SCIENCE AND TECHNOLOGY IRELAND LIMITED;O'SULLIVAN, SUSAN;O'NEILL, JOHN