Method for production of 4,10beta-diacetoxy-2$g(a)-benzoyloxy-5$g(b),20-epoxy-1,13$g(a)-dihydroxy-9-oxo-19-norcyclopropa[g]tax-11-ene

Preparation of taxoid compounds (I) comprises reacting an optionally protected taxene compound (II) with a molecular sieve base in sulfolane, condensing with a side chain, and removing protecting groups. Preparation of taxoid compounds of formula (I) comprises reacting an optionally protected taxene...

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Bibliographic Details
Main Authors GUY AMOURET, ERIC DIDIER
Format Patent
LanguageEnglish
Published 28.10.2004
Edition7
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:Preparation of taxoid compounds (I) comprises reacting an optionally protected taxene compound (II) with a molecular sieve base in sulfolane, condensing with a side chain, and removing protecting groups. Preparation of taxoid compounds of formula (I) comprises reacting an optionally protected taxene compound of formula (II) with a basic molecular sieve in sulfolane to cyclize the 7 beta -trifluoromethyl sulfonyloxy group, condensing with a side chain, and removing protecting groups. [Image] Ar : aryl; R : H, acetyl, alkoxyacetyl or alkyl; R 1benzoyl or R 2-O-CO; R 21-8C alkyl; R' : a protecting group when R in (I) is H, or R. An independent claim is also included for the preparation of intermediate compounds of formula (III) which comprises reacting (II) with a molecular sieve base in sulfolane. [Image] ACTIVITY : None given. MECHANISM OF ACTION : None given.
Bibliography:Application Number: AU20040230302