Process for the esterification of baccatin III and of 10-deacetylbaccatin III
US5717103A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Apr 5, 1995 |
| Grant date | Feb 10, 1998 |
| Priority date | — |
| Expiry date | Apr 5, 2015 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02P20/55
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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##
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.