VERFAHREN ZUR HERSTELLUNG VON TAXAN-DERIVATEN

摘要

PCT No. PCT/FR93/00969 Sec. 371 Date Apr. 5, 1995 Sec. 102(e) Date Apr. 5, 1995 PCT Filed Oct. 4, 1993 PCT Pub. No. WO94/07879 PCT Pub. Date Apr. 14, 1994This 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, R1 is a benzoyl radical or an R2-O-CO- radical in which R2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R3 is a trihalomethyl radical or phenyl substituted by a trihalomethyl radical, R4 is a hydrogen atom or is the same as R1. (I) (VII)