Novel process for preparing a 5-hydroxy-3-oxo-hexanoic acid...

C - Chemistry – Metallurgy – 07 – C

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C07C 67/343 (2006.01) C07C 51/353 (2006.01) C07C 59/90 (2006.01) C07C 69/716 (2006.01)

Patent

CA 2512630

The present invention is related to a novel process for preparing an optically active 5-hydroxy-3-oxo-hexanoic acid derivative or its tautomer which is useful intermediate for preparing statins such as atorvastatin and rosuvastatin. Blaise reaction of (S)-4-halo-3 -hydroxybutyronitrile with - haloacetate is utilized as a key reaction to provide the product with minimal formation of side products and in good yield.

L'invention concerne un nouveau procédé pour préparer un dérivé d'acide 5-hydroxy-3-oxo-hexanoïque optiquement actif, ou son tautomère, qui constitue un intermédiaire utile pour préparer des statines, notamment l'atorvastatine et la rosuvastatine. Une réaction de Blaise de <= <I>S</I> >=-4-halo-3-hydroxybutyronitrile avec de l'alpha-haloacétate, est utilisée en tant que réaction clé pour obtenir le produit avec une formation minimale de produits secondaires, et ce avec un bon rendement.

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