Method for preparing taxane derivatives

This invention relates to a method for preparing taxane derivatives of general formula (I)by esterification at a temperature between -10 and 60° C. of a derivative of baccatine III or 10-deacetyl baccatine III of general formula (II)by means of an acid of general formula (III),followed by replacemen...

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Bibliographic Details
Main Authors ELIE FOUQUE, JEAN-MANUEL MAS
Format Patent
LanguageEnglish
Published 05.02.1998
Edition6
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:This invention relates to a method for preparing taxane derivatives of general formula (I)by esterification at a temperature between -10 and 60° C. of a derivative of baccatine III or 10-deacetyl baccatine III of general formula (II)by means of an acid of general formula (III),followed by replacement of the protective groupings G1, G2 and R2 of the resulting product by hydrogen atoms. In formulae (I), (II) or (III), Ar stands for an aryl radical; R stands for hydrogen or acetyl; R1 is benzoyl or ter.butoxycarbonyl; G1 is a hydroxy function protective grouping, G2 stands for the acetyl radical or a hydroxy function protective grouping, and R2 stands for a hydroxy function protective grouping.
Bibliography:Application Number: AU19930035048