Process for the preparation of taxane derivatives

Details Process for the preparation of taxane derivatives Process for the preparation of taxane derivatives

1997-01-03

1998-03-10

Trinh, Ba K.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

549510, 549511, C07D26306, C07D30514

Patent

active

057263183

ABSTRACT:
This 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, R.sub.1 is a benzoyl radical or an R.sub.2 --O--CO-- radical in which R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R.sub.3 is a trihalomethyl radical or phenyl substituted by a trihalomethyl radical, R.sub.4 is a hydrogen atom or is the same as R.sub.1. ##STR1##

REFERENCES:
patent: 5319112 (1994-06-01), Kingston et al.
patent: 5556878 (1996-09-01), Kelly et al.
patent: 5580997 (1996-12-01), Bouchard et al.
Gueritte-Voegelein et al. "Relationships between the structure of Taxol Analogues and Their Antimitotic Activity", J. Med. Chem. 1991, 34, 992-998 .

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