Taxoids, their preparation and the pharmaceutical compositions w

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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549511, C07D30514

Patent

active

056544499

ABSTRACT:
This invention relates to a process for preparing taxoid derivatives of formulae II and XI: ##STR1## in which Ar represents an aryl radical; R.sub.1 represents a benzoyl radical or a radical R.sub.2 --O--CO-- in which R.sub.2 represents an unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl, or saturated or unsaturated heterocyclic radical; R.sub.3 represents an unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, saturated or unsaturated heterocyclic, or aryl radial, but not a phenyl radical; R.sub.4 represents a hydrogen atom and R.sub.5 represents a hydroxyl-protecting group or R.sub.4 and R.sub.5 together form a heterocyclic group; G.sub.1 represents a hydroxyl-protecting group; and G.sub.2 represents an acetyl radical or hydroxyl-protecting group;
by electrolytically reducing a protected taxoid compound in an electrolyte comprising a quaternary ammonium salt which is soluble in an organic solvent or in an aqueous/organic mixture at a controlled potential.

REFERENCES:
patent: 5254703 (1993-10-01), Holton
patent: 5430160 (1995-07-01), Holton

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