Process for purifying 20(s)-camptothecine

Details Process for purifying 20(s)-camptothecine Process for purifying 20(s)-camptothecine

C - Chemistry, Metallurgy

07

D

C07D 491/04 (2006.01) C07D 491/14 (2006.01) C07D 491/22 (2006.01)

Patent

CA 2435372

The invention relates to a method for purifying 20(S) camptothecine: (see formula I) wherein R1 is ethyl, by transforming the lactone ring of the 20(S) camptothecine into a carboxylate salt with the help of an aqueous base, hydrogenating the mixture that is obtained in the presence of a transition metal catalyst, acidifying the aqueous phase to form camptothecine crystals, adding a polar aprotic solvent, optionally heating and cooling the mixture and separating the camptothecine crystals.

Procédé de purification de 20(S)-camptothécine, qui consiste à transformer le noyau lactone de la 20(S)-camptothécine en un sel de carboxylate à l'aide d'une base aqueuse, à hydrogéner le mélange obtenu en présence d'un catalyseur à base de métaux de transition, à acidifier la phase aqueuse, ce qui entraîne la formation de cristaux de camptothécine, à ajouter un solvant polaire aprotique, éventuellement à chauffer et à refroidir le mélange et à séparer les cristaux de camptothécine.

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