C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 491/10 (2006.01) A61K 31/55 (2006.01) A61P 25/28 (2006.01)
Patent
CA 2674300
The invention relates to a method for the production of high-purity galanthamine, or high-purity galanthamine derivatives, wherein racemic bromine narwedine is utilized as a base, which is debrominated under palladium catalysis. The processing of the reaction mixture is substantial to the invention and is carried out in the presence of oxygen or peroxides such that the palladium catalyst is transferred into an insoluble, easy to cleave form. The subsequent reaction is carried out by means of the reduction of enantiomer-pure narwedine into enantiomer-pure galanthamine, wherein alylating or dealkylating takes place subsequently such that a corresponding substitution is achieved at the ring nitrogen atom. Residual amounts of palladium of below 5 ppm are obtained by further purification, such as recrystallization, such that the direct use as a pharmaceutical raw material is enabled.
La présente invention concerne un procédé de production de galantamine très pure ou de dérivés de galantamine très pure à partir de narwédine de brome racémique qui est débromée par catalyse au palladium. Selon l'invention, le traitement du mélange réactionnel a lieu en présence d'oxygène ou de peroxydes, de manière que le catalyseur au palladium soit transformé sous une forme insoluble facilement séparable. La réaction ultérieure consiste en une réduction de narwédine énantiopure en galantamine énantiopure, puis en une alkylation ou une désalkylation, permettant d'obtenir une substitution correspondante au niveau de l'atome d'azote du cycle. Une purification ultérieure, telle qu'une recristallisation, permet d'obtenir des résidus de palladium à moins de 5 ppm, autorisant ainsi une utilisation directe comme matière première pharmaceutique.
Gerdenitsch Anton
Kolar Susanne
Rothenburger Jan
Scherleithner Alexandra
Welzig Stefan
Borden Ladner Gervais Llp
Sanochemia Pharmazeutika Ag
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