Stragen Pharma Sa

Oncopharm Corporation

Ludovic Chauviat

Jean-Pierre Robin

Robert Dhal

Julie Blanchard

Chrystelle Gilet

Sylvie Cavoleau

Sandrine Poutot

Laurent Girodier

Laurence Mevelec

Gilles Dujardin

Sylvie Rouaud

Sandra Charbonnel

Florence Fournier

Jean-Pierre Marie

Nina Radosevic

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%.

Cephalotaxane derivatives and their processes of preparation and purification

The present invention concerns a new general process for asymetric hemisynthesis of harringtonines and their analogs, that are alcaloids used in chimiotherapy. This process comprises direct esterification of a natural cephalotaxine with an acylating compound constituted of a side chain precursor which backbone and fonctionalization are entirely preformed.

Cephalotaxane derivatives and process for their preparation

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Le Mans, France

Ludovic Chauviat