Process for the esterification of baccatin III and of 10-deacetylbaccatin III
Number of patents in Portfolio can not be more than 2000
United States of America Patent
Stats
-
Feb 10, 1998
Grant Date -
N/A
app pub date -
Apr 5, 1995
filing date -
Oct 5, 1992
priority date (Note) -
In Force
status (Latency Note)
Importance
Abstract
This invention relates to a method of preparing esters of baccatine III or 10-deacetylbaccatine III of formula (I) by esterification of protected baccatine III or 10-deacetylbaccatine III of formula (II) by means of an activated acid of formula (III). The esters of formula (I) can be used to prepare taxane derivatives having remarkable antileucemia and antitumor properties. In formulae (I), (II) and (III) Ar is an aryl radical, R.sub.1 is a hydrogen atom or an aryl radical or an R.sub.4 --O--CO-- radical (R.sub.4 =alkenyl, alkynyl, optionally substituted alkyl, cycloalkyl, cycloalkynyl, bicycloalkyl, phenyl, heterocyclyle) and R.sub.2 is a hydrogen atom, and R.sub.3 stands for a hydroxy function protection grouping, or R.sub.1 is defined as above and R.sub.2 and R.sub.3 together form a 5 or 6 membered, saturated heterocyclic ring, G.sub.1 is an acetyl radical or a hydroxy function protection grouping, G.sub.2 is a hydroxy function protection grouping, and X is an acyl radical, aryl, radical or halogen atom. ##STR1##
First Claim
Family
International Classification(s)
Cited Art Landscape
Patent Citation Ranking
Advertisement
Advertisement
Advertisement
Recipient Email Address
Recipient Email Address
Comment
Recipient Email Address
Add to Portfolio(s)
To add this patent to one, or more, of your portfolios, simply click the add button.
This Patent is in these Portfolios:
Add to additional portfolios:
Last Refreshed On:
Changes done successfully