Cephalotaxane derivatives and their processes of preparation and purification
US7842687B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | May 25, 2006 |
| Grant date | Nov 30, 2010 |
| Priority date | — |
| Expiry date | May 29, 2029 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D453/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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: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%.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.