Novel method for preparing taxane derivatives, novel derivatives thus obtained and compositions containing them

摘要

PCT No. PCT/FR93/01145 Sec. 371 Date May 23, 1995 Sec. 102(e) Date May 23, 1995 PCT Filed Nov. 22, 1993 PCT Pub. No. WO94/12484 PCT Pub. Date Jun. 9, 1994This invention relates to a method for the preparation of taxane derivatives having the formula (I) and pharmaceutical compositions which contain the derivatives thus obtained. In formula (I), R is hydrogen or acetyl, R1 is benzoyl or R2-O-CO wherein R2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl and Het is a 5-membered optionally substituted aromatic heterocycle (thiophene, tiazole, furan, pyrrole, imidazole, oxazole, isoxazole, pyrazole). The products of formula (I) have remarkable antitumor and antileukemia properties. (I)