Semi-synthetic conversion of paclitaxel to docetaxel

Details Semi-synthetic conversion of paclitaxel to docetaxel Semi-synthetic conversion of paclitaxel to docetaxel

C - Chemistry, Metallurgy

07

D

C07D 305/14 (2006.01)

Patent

CA 2572315

A process is provided for the semi-synthesis of taxane derivatives useful in the preparation of docetaxel, in particular, the semi-synthesis of protected taxane derivatives in a one pot reaction of protecting the C-2', C-7 and C-10 and introducing a t-Boc group at the nitrogen of the amide group at the C-3' position in paclitaxel and subsequently conversion to docetaxel, and derivatives used therein.

La présente invention concerne un processus de semi-synthèse de dérivés de taxane qui convient pour la préparation de docetaxel, en particulier, la semi-synthèse de dérivés de taxane protégés dans une réaction en un pot, la protection en C-2', C-7 et C-10, et l'introduction d'un groupe t-Boc au niveau de l'azote du groupe amide en position C-3' dans le paclitaxel et, ensuite, la conversion en docetaxel. Cette invention concerne aussi des dérivés utilisés dans ce processus.

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