Rhone-poulenc Rorer S.a.

Aventis Pharma S.a.

Elie Fouque

Alain Commercon

Eric Didier

Jean-Manuel Mas

Jean-Rene Authelin

Isidore Le Fur

Bernadette Mandard

Claude Bertrand

Jean-Paul Richard

Isabelle Taillepied

Jacques Doveze

Method for preparing taxane derivatives

Process for the preparation of 4-acetoxy-2.alpha.-benzoyloxy-5.beta.,

This invention relates to a method of preparing taxane derivatives of formula (VIII) by esterification of protected baccatin III or 10-deacetylbaccatin III by means of an acid of formula (VII), elimination of protection groupings and acylation of the amine function of the side chain. In formulae (VIII) and (VII): Ar stands for aryl, R.sub.3 is a trihalomethyl radical or phenyl substituted by a trihalomethyl radical, R.sub.4 is a hydrogen atom or is the same as R.sub.1. G.sub.1 and G.sub.2 are hydroxy protecting groups. ##STR1##

Process for the preparation of taxane derivatives

This invention relates to a method of preparing taxane derivatives of formula (I) by esterification of protected baccatin III or 10-deacetylbaccatin III by means of an acid of formula (VII), elimination of protection groupings and acylation of the amine function of the side chain. The products of formula (I) have remarkable antitumor and antileukemia properties. In formulae (I) and (VII): Ar stands for aryl, R is hydrogen or acetyl, R.sub.1 is a benzoyl radical or an R.sub.2 --O--CO-- radical in which R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R.sub.3 is a trihalomethyl radical or phenyl substituted by a trihalomethyl radical, R.sub.4 is a hydrogen atom or is the same as R.sub.1. ##STR1##

Process for preparing taxane derivatives

Process for transforming (benzoyl-3-phenyl)-2-propionic-R(-) acid into an S(+) isomer through the action of a base either in situ during the splitting of racemic ketoprofen or on the crystallization mother liquor of a (benzoyl-3-phenyl)-2-propionic-S(+) acid salt.

Process for converting [R(-)-2(3-benzoylphenyl)-propionic acid to the

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Saint Maur des Fosses, France

Elie Fouque