Method for preparing taxane derivatives
AssigneeRhone-Poulenc Rorer S.A.
InventorsJean-Noel Denis, Andrew-Elliot Greene, Alice Kanazawa
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AssigneeRhone-Poulenc Rorer S.A.
InventorsJean-Noel Denis, Andrew-Elliot Greene, Alice Kanazawa
Estimating the term…
A method for preparing taxane derivatives of general formula (I) by esterifying protected baccatin III or protected 10-deacetyl baccatin III with an acid of general formula (II). In general formulae (I) and (II), Ar is an aryl radical; R.sub.1 and R.sub.2 which are the same or different, are a hydrogen atom, an alkyl, phenylalkyl, phenyl, alkoxyphenyl or dialkoxyphenyl radical, or R.sub.1 or R.sub.2, together with the carbon atom to which they are attached, form a 4-7 membered ring; R.sub.3 is an acetyl radical or a hydroxy function protective grouping, and R.sub.4 is a hydroxy function protective grouping; R is a phenyl radical or a radical of formula R.sub.5 --O-- wherein R.sub.5 -- is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl or saturated or unsaturated nitrogenous heterocylcyl radical. The products of general formula (I) are particularly useful for preparing taxol, Taxotere and analogues thereof having remarkable antitumor properties. ##STR1##
A process for preparing a taxane derivative of formula I:
The process according to claim 1, wherein the esterification is carried out with an acid of formula (VI):
Dependencies are inferred from the claim text.