Process for the preparation of taxane derivatives

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

1997-10-31

1999-01-19

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

058615156

ABSTRACT:
This invention relates to a method of preparing taxane derivatives of formula (VIII) 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. In formulae (VIII) and (VII): Ar stands for aryl, 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. G.sub.1 and G.sub.2 are hydroxy protecting groups. ##STR1##

REFERENCES:
patent: 5319112 (1994-06-01), Kingston et al.
patent: 5621121 (1997-04-01), Commercon
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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