NOVOS DERIVADOS DE CEFALOTAXANOS E PROCESSO PARA A SUA PREPARACAO

The present invention concerns a new general process for asymmetric hemisynthesis of harringtonines and their analogs, that are alkaloids used in chemotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor whi...

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Hauptverfasser: CHAUVIAT, LUDOVIC, POUTOT, SANDRINE, CHARBONNEL, SANDRA, GIRODIER, LAURENT, GILET, CHRYSTELLE, DUJARDIN, GILLES, ROBIN, JULIE, JEAN-PIERRE ROBIN, ROUAUD, SYLVIE, ROBERT DHAL, CAVOLEAU, SYLVIE, MEVELEC, LAURENCE, FOURNIER, FLORENCE
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creator CHAUVIAT, LUDOVIC
POUTOT, SANDRINE
CHARBONNEL, SANDRA
GIRODIER, LAURENT
GILET, CHRYSTELLE
DUJARDIN, GILLES
ROBIN, JULIE
JEAN-PIERRE ROBIN
ROUAUD, SYLVIE
ROBERT DHAL
CAVOLEAU, SYLVIE
MEVELEC, LAURENCE
FOURNIER, FLORENCE
description The present invention concerns a new general process for asymmetric hemisynthesis of harringtonines and their analogs, that are alkaloids used in chemotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor which backbone and functionalization are entirely preformed. The invention also concerns a natural, synthetic or semi-synthetic harringtonines including their tautomeric forms and their salts of the following formula: wherein n=2 (i.e. harringtonine) or n=3 (i.e. homoharringtonine), in which the total content of impurities, possibly including enantiomeric forms, is lower than 1%, and/or the content of the major impurity is lower than 0.9%, and/or the chromatographic assay exhibits a harringtonines content higher than 97.5%.
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subjects ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title NOVOS DERIVADOS DE CEFALOTAXANOS E PROCESSO PARA A SUA PREPARACAO
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