COMBRETASTATIN DERIVATIVE PREPARATION METHOD

The invention relates to a method for preparing a combretastatin derivative (I) or (II), said method including the following steps: triaryl(3,4,5-trimethoxybenzyl)phosphonium halide P3 (III), wherein Ar denotes an aryl group selected from among phenyl or thienyl, is reacted with P2 having formula (I...

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Bibliographic Details
Main Authors PASCAL BESSE, ERIC DIDIER, NICOLAS TREMAUDEUX
Format Patent
LanguageEnglish
Spanish
Published 19.06.2012
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:The invention relates to a method for preparing a combretastatin derivative (I) or (II), said method including the following steps: triaryl(3,4,5-trimethoxybenzyl)phosphonium halide P3 (III), wherein Ar denotes an aryl group selected from among phenyl or thienyl, is reacted with P2 having formula (IV) or P'2 having formula (V) so as to respectively obtain the compound P4 or P'4, which have formulas (VI) and (VII), respectively; then, during a step for deprotection in the presence of an acid and/or a base, the compound having P4 or P'4 leads, after an optional purification step, to the compound having formula (I) or (II). La invención se refiere a un procedimiento de preparación de un derivado de combretastatina (I) ó (II): que comprende las etapas siguientes: se hace reaccionar el halogenuro de triaril(3,4,5-trimetoxibencil)fosfonio P3 (III) en donde Ar significa un grupo arilo seleccionado entre fenilo o tienilo, con P2 de fórmula (IV) o bien P'2 de fórmula (V) con el fin de obtener, respectivamente, el compuesto P4 ó P'4: luego, en el transcurso de una etapa de desprotección en presencia de un ácido y/o de una base, el compuesto de fórmula P4 ó P'4 conduce, después de una etapa eventual de purificación, al compuesto de fórmula (I) ó (II).
Bibliography:Application Number: MX20120006388