Rhone-poulenc Rorer S.a.

Centre National De La Recherche Scientifique

Aventis Pharma S.a.

Jean-Noel Denis

Andrew-Elliot Greene

Alice Kanazawa

Andrew E Greene

Jean-Manuel Mas

Arlene Correa

Arlene G Correa

Daniel Guenard

Francoise Gueritte-Voegelein

David S Grierson

Novel carboxylic acids of formula (VI), useful for preparing taxane derivatives of general formula (I) by esterifying protected baccatine (III) or protected diacetyl baccatin (III) with an acid of general formula (II). The products of general formula (I) are particularly useful for preparing taxol, Taxotere and analogs thereof having anti-tumor properties.

Carboxylic acids for synthesis of taxane derivatives

A .beta.-phenylisoserine derivative of general formula (I): ##STR1## in the form of a salt or an ester, in which Ar represent an aryl radical, R represents a phenyl or naphthyl or a O--R.sub.1 radical and G.sub.1 represents --CH.sub.2 --Ph radical; and a method of using the same for making taxane derivatives.

Method for the stereo-selective preparation of a derivative of

A compound of the formula I: ##STR1## wherein Ar represents an aryl radical;

Esters of baccatin III and 10-deacetylbaccatin III

Process for the preparation of a 1,3-oxazolidine-5-carboxylic acid

Process for the stereoselective preparation of a .beta.-phenylisoserine

Process for the esterification of baccatin III and of

Method for preparing taxane derivatives

Process for the enantioselective preparation of phenylisoserine derivatives of general formula (I), in which R represents a phenyl or tert-butoxy radical, R.sub.1 represents a hydrogen atom or an alkyl radical containing 1 to 4 carbon atoms and R.sub.2 represents a hydrogen atom or a group protecting the alcohol function. ##STR1##

Process for the enantioselective preparation of phenylisosrine

Process for the enantioselective preparation of phenylisoserine

Process for the stereoselective preparation of phenylisoserine

Process for preparing taxol by the condensation of a (2R, 3S) acid of general formula (I) with a taxan derivative of general formula (II), followed by the removal of the groups R.sub.2 and R.sub.3 protecting the hydroxy groups. ##STR1##

Process for preparing taxol

Growing community of inventors

Uriage, France

Jean-Noel Denis