Method for preparing...

C - Chemistry – Metallurgy – 07 – J

Patent

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Details

C07J 41/00 (2006.01) A61K 9/16 (2006.01) A61K 31/567 (2006.01) A61P 5/36 (2006.01) C07J 1/00 (2006.01) C07J 75/00 (2006.01)

Patent

CA 2648537

The present invention relates to a method for the reliable and reproducible preparation of 4-[17.beta.-methoxy-17.alpha.-methoxymethyl-3-oxoestra-4,9-dien-ll.beta.- yl]benzaldehyde (E)-oxime (asoprisnil) on the pilot and manufacturing scale. Asoprisnil, which is prepared by this method, is distinguished by a very good physical stability and is therefore particularly suitable for the manufacture of solid pharmaceutical forms (tablets, coated tablets, etc.).

L'invention porte sur une méthode de préparation de 4-[17.beta.-methoxy-17.alpha.-méthoxyméthyl-3-oxoestra-4,9-dien-11.beta.-yl]benzaldéhyde (e)-oxime (asoprisnil) à l'échelle pilote et à l'échelle de fabrication. L'asoprisnil, préparé par cette méthode, qui se distingue par une très bonne stabilité physique, est donc particulièrement adapté à la fabrication de formes pharmaceutiques solides (comprimés, comprimés pelliculés, etc.).

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