Generated: May 29, 2017
|Title:||Cephalotaxane derivatives and their processes of preparation and purification|
|Abstract:||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: ##STR00001## 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%.|
|Inventor(s):||Robin; Jean-Pierre (Nyon, CH), Blanchard; Julie (Rouillon, FR), Marie; Jean-Pierre (Sevres, FR), Radosevic; Nina (Nyon, CH)|
|Assignee:||Chemgenex Pharmaceuticals, Inc. (Geelong, Victoria, AU)|
Patent Claim Types:|
see list of patent claims
|Compound; Composition; Use;|
|Foriegn Application Priority Data|
|Foreign Country||Foreign Patent Number||Foreign Patent Date|
|France||98 03492||Mar 20, 1998|
|Country||Document Number||Estimated Expiration||Supplementary Protection Certificate||SPC Country||SPC Expiration|
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