The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Feb. 09, 1999

Filed:

Aug. 08, 1997
Applicant:
Inventors:

Jean-Manuel Mas, Villeurbanne, FR;

Viviane Massonneau, Ecully, FR;

Assignee:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D / ; C07D / ;
U.S. Cl.
CPC ...
548215 ; 548216 ; 549510 ; 549511 ;
Abstract

This invention relates to a 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, R.sub.1 is benzoyl or R.sub.2 -CO--O- in which R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R.sub.3 and R.sub.4 may be the same or different and represent hydrogen, alkyl, alkenyl, aralkyl, aryl or alkoxy, and R.sub.5 is an alkyl radical substituted by one or more chlorine atoms (2,2,2-trichloroethyl, 2-trichloromethylisopropyl). ##STR1##


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