An improved preparation of atorvastatin

Details An improved preparation of atorvastatin An improved preparation of atorvastatin

C - Chemistry, Metallurgy

07

D

C07D 207/34 (2006.01) C07D 207/416 (2006.01)

Patent

CA 2460935

A process for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl- 4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, tert- butylester comprising: (a) reduction of 5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4- [(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-oxo-1-pentanoic acid, (R)- 2-hydroxy-1,2,2-triphenylethyl ester; (b) hydrolysis of (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4- [(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (R)-2-hydroxy-1,2,2-triphenylethyl ester using an alkali base in a solvent to form the acid; (c) alkylation of the acid forming (R)-5-[2-(4-fluorophenyl)-5-(1- methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5- hydroxy-3-oxo-1-heptanoic acid, tert-butylester.

Divulgation d'un procédé de préparation de (R)-5-¬2-(4-fluorophényl)-5-isopropyl-3-phényl- 4-¬(phénylamino)carbonyl|-1H-pyrrol-1-yl|-5-hydroxy-3-oxo-1-heptanoate de tert-butyle. Ce procédé comprend : a) la réduction du 5-¬2-(4-fluorophényl)-5-isopropyl-3-phényl-4- ¬(phénylaminocarbonyl|-1H-pyrrol-1-yl|-3-oxo-1-pentanoate de (R)-2-hydroxy-1,2,2-triphényléthyle, b) l'hydrolyse du (R)-5-¬2-(4-fluorophényl)-5-isopropyl-3-phényl-4-¬(phénylamino)carbonyl|-1H-pyrrol-1-yl|-3-hy droxy-1-pentanoate de (R)-2-hydroxy-1,2,2-triphényléthyle au moyen d'un alcali dans un solvant pour former l'acide, c) l'alkylation de l'acide pour former le (R)-5-¬2-(4-fluorophényl)-5-isopropyl-3-phényl-4-¬(phénylamino)carbonyl|-1H-pyrrol-1-yl|-5- hydroxy-3-oxo-1-heptanoate de tert-butyle.

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