Processes for preparing calcium salt forms of statins

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 207/34 (2006.01) A61K 31/366 (2006.01) A61K 31/40 (2006.01) A61K 31/47 (2006.01) A61K 31/505 (2006.01) C07D 215/14 (2006.01) C07D 239/42 (2006.01) C07D 309/30 (2006.01)

Patent

CA 2450820

Processes for preparing a calcium salt of a statin from an ester derivative or protected ester derivative of the statin by using calcium hydroxide are provided. The ester or protected ester derivative is contacted with calcium hydroxide to obtain the calcium salt. Preferred statins are rosuvastatin, pitavastatin and atorvastatin, simvastatin and lovastatin. In processes beginning with a protected satin ester derivative, the protecting group is hydrolyzed during salt formation by contact with calcium hydroxide, or is contacted with an acid catalyst followed by contact with calcium hydroxide.

L'invention concerne des procédés permettant de préparer un sel calcique d'une statine à partir d'un dérivé d'ester ou d'un dérivé d'ester protégé de la statine au moyen d'hydroxyde de calcium. Le dérivé d'ester ou le dérivé d'ester protégé est mis en contact avec l'hydroxyde de calcium pour obtenir le sel calcique. Les statines préférées sont la rosuvastatine, la pitavastatine et l'atorvastatine, la simvastatine et la lovastatine. Dans les procédés qui commencent avec un dérivé d'ester de statine protégé, le groupe protecteur est soit hydrolysé pendant la formation du sel par contact avec l'hydroxyde de calcium, soit mis en contact avec un catalyseur acide, puis avec l'hydroxyde de calcium.

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