Method for the preparation of morphine compounds

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 489/00 (2006.01) A61K 31/485 (2006.01) A61P 29/00 (2006.01) C07B 63/02 (2006.01) C07D 489/08 (2006.01)

Patent

CA 2705251

The present invention relates to a method for the preparation of morphine compounds comprising a low content of a,ß-unsaturated compounds, which comprises the steps of: (i) bringing the crude morphine compound into contact with a base, at a pH of greater than 13, under conditions which make possible the Michael addition reaction on the a,ß-unsaturated compound(s) present; (ii) separating the morphine compound from the reaction mixture; and (iii) if appropriate, separating the addition product formed, from the morphine compound. It also relates to a composition comprising at least 99% by dry weight of morphine compound, or of a pharmaceutically acceptable salt thereof, and an a,ß-unsaturated compound in a content of less than 100 ppm.

La présente invention concerne un procédé de préparation de composés morphiniques à faible teneur en composés .alpha.-.beta. insaturés, comportant les étapes de: (i) mise en contact du composé morphinique brut avec une base, à pH supérieur à 13 et dans des conditions permettant la réaction d'addition de Michael sur le(s) composé(s) .alpha.-.beta. insaturés présents; (ii) séparation du composé morphinique du mélange réactionnel; et (iii) le cas échéant, séparation du produit d'addition formé du composé morphinique. Elle vise également une composition comprenant au moins 99 % en poids sec de composé morphinique ou d'un de ses sels pharmaceutiquement acceptables et un composé .alpha.-.beta.-insaturé en une teneur inférieure à 100 ppm.

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