METHOD OF PREPARING TAXANE DERIVATIVES, AND INITIAL AND INTERMEDIATE PRODUCTS FOR PREPARATION THEREOF

摘要

FIELD: medicine. SUBSTANCE: present invention describes method of preparing taxane derivatives of formula (I) by esterifying protected baccatine III or 10-deacety- bacctine III using acid of formula (VII), removing protecting groups and subsequently acylating functional amino groups of side unit. Compounds of formula (I) have antitumor and antileukemic properties. In formula (I) and formula (VII) Ar is phenyl; R is hydrogen or acetyl; R1 is benzoyl or R2-O-CO- in which R2 is straight or branched C1-C8-alkyl; R3 is trihalomethyl; R4 is hydrogen atom or is identical with R1 substitute. EFFECT: improved properties of taxane derivatives. 26 cla