Process for preparing taxane derivatives

Details Process for preparing taxane derivatives Process for preparing taxane derivatives

C - Chemistry, Metallurgy

07

D

C07D 305/14 (2006.01) C07D 263/04 (2006.01) C07D 263/06 (2006.01) C07D 401/12 (2006.01) C07D 405/12 (2006.01) C07D 413/12 (2006.01)

Patent

CA 2146250

Method of preparing taxane derivatives of general formula (I) by esterification of protected baccatine III or 10-deacetylbaccatine III by means of an acid of general formula (VII), elimination of protection groupings of the ester obtained, and acylation of the amine function of the side chain. In formulae (I) and (VII): Ar stands for aryl, R is hydrogen or acetyl, R1 is benzoyl or R2-O-CO- in which R2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R3 and R4 may be the same or different and represent hydrogen, alkyl, alkenyl, aralkyl, aryl or alkoxy, and R5 is an alkyl radical substituted by one or more chlorine atoms (2,2,2-trichloroethyl, (2-trichloromethylisopropyl).

Procédé de préparation de dérivés du taxane de formule générale (I) par estérification de la baccatine III ou de la désacé- tyl-10 baccatine III protégée au moyen d'un acide de formule générale (VII), élimination des groupements protecteurs de l'ester obtenu puis acylation de la fonction amine de la chaîne latérale. Dans les formule (I) et (VII): Ar représente aryle, R représente hydrogène ou acétyle, R1 représente benzoyle ou R2-O-CO- dans lequel R2 représente alcoyle, alcényle, alcynyle, cycloal- coyle, cycloalcényle, bicycloalcoyle, phényle ou hétérocyclyle, R3 et R4, identiques ou différents, représentent hydrogène, al- coyle, alcényle, aralcoyle, aryle ou alcoxy, et Rg représente un radical alcoyle substitué par un ou plusieurs atomes de chlore (trichloro-2,2,2 éthyle), (trichlorométhyl-2 isopropyle).

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