Process for the preparation of taxane derivatives

Taxane derivatives of formula (I) are prepared by esterification of protected baccatin III or protected 10-deacetyl-baccatin III with an acid of formula (VII) removal of the protective groups and acylation of the amine functional group of the side chain. The products of formula (I) have notable anti...

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Bibliographic Details
Main Authors DIDIER, ERIC, COMMERCON, ALAIN, FOUQUE, ELIE
Format Patent
LanguageEnglish
Published 11.06.2000
Edition7
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:Taxane derivatives of formula (I) are prepared by esterification of protected baccatin III or protected 10-deacetyl-baccatin III with an acid of formula (VII) removal of the protective groups and acylation of the amine functional group of the side chain. The products of formula (I) have notable antitumour and antileukaemic properties. In formula (I) and (VII), Ar represents aryl. R represents hydrogen or acetyl, R1 represents a benzoyl radical or a radical R2-O-CO- in which R2 represents alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R3 represents trihalomethyl or phenyl substituted by trihalomethyl R4 represents hydrogen or is identical to R1.
Bibliography:Application Number: TW199382108100