A process for the preparation of a taxane derivative

Details A process for the preparation of a taxane derivative A process for the preparation of a taxane derivative

C - Chemistry, Metallurgy

07

D

C07D 493/10 (2006.01) A61K 31/357 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2652008

The invention relates to an improved process for the synthesis of 13-(N- Boc-.beta.-isobutylserinyl)-14-.beta.-hydroxybaccatin III-1,14-carbonate (I), wherein carbonation of the 1,14-hydroxy groups of the baccatin skeleton is carried out with bis(trichloromethylcarbonate and the 7-hydroxy group is protected with a trichloroacetyl group.

L'invention concerne un procédé amélioré pour la synthèse de 13-(N-Boc-.beta.-isobutylsérinyl)-14-.beta.-hydroxybaccatine III-1,14-carbonate (I). Selon ce procédé, la carbonation des groupes 1,14-hydroxy du squelette de baccatine est réalisée avec du bis(trichlorométhylcarbonate) et le groupe 7-hydroxy est protégé avec un groupe trichloroacétyle.

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