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Generated: December 13, 2017

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Title: Cephalotaxane derivatives and process for their preparation
Abstract: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.
Inventor(s): Robin; Jean-Pierre (Le Mans, FR), Blanchard; Julie (Le Mans, FR), Cavoleau; Sylvie (Angers, FR), Chauviat; Ludovic (Le Mans, FR), Charbonnel; Sandra (Angers, FR), Dhal; Robert (Pruille le Chetif, FR), Dujardin; Gilles (Rouillon, FR), Fournier; Florence (Le Mans, FR), Gilet; Chrystelle (Le Mans, FR), Girodier; Laurent (Le Mans, FR), Mevelec; Laurence (Louvier, FR), Poutot; Sandrine (Le Mans, FR), Rouaud; Sylvie (Le Mans, FR)
Assignee: Stragen Pharma SA. (Geneva, CH)
Filing Date:Mar 16, 1999
Application Number:09/270,006
Claims:1. A compound of formula: ##STR156##

wherein n is between 2 or 3, R.sub.5 represents hydrogen, --CH.sub.2 COOH, --CH.sub.2 COOMe(--CH.sub.2 COOH.sub.3), --CH.sub.3, --OH, --OMe(--OCH.sub.3) or --CH.sub.2 CH.sub.3, and R.sub.6 and R.sub.8 are independently hydrogen or phenyl but may not be both hydrogen, and may be further independently --CH.sub.3 when R.sub.5 represents --CH.sub.2 COOH or --CH.sub.2 COOMe(--CH.sub.2 COOH.sub.3), or one of its salts, or each one of its pure enantiomeric forms or in racemic mixture or in variable composition.

2. The compound of claim 1, wherein R.sub.5 represents hydrogen or --CH.sub.2 COOCH.sub.3.

3. The compound of claim 1, or one of its salts, or each one of its pure enantiomeric forms or in racemic mixture or in variable composition, corresponding to the following formula: ##STR157##

4. The compound of claim 1, or one of its salts, or each one of its pure enantiomeric forms or in racemic mixture or in variable composition, corresponding to the following formula: ##STR158##

5. The compound of claim 1, corresponding to the following formula: ##STR159##

or one of its salts, or each one of its pure enantiomeric forms or in racemic mixture or in variable composition.

6. A compound of formula: ##STR160##

or one of its salts, or each one of its pure enantiomeric forms or in racemic mixture or in variable composition.

7. A compound of formula: ##STR161##

or one of its salts, or each one of its pure enantiomeric forms or in racemic mixture or in variable composition.

8. A compound of formula: ##STR162##

or one of its salts, or each one of its pure enantiomeric forms or in racemic mixture or in variable composition.

9. A compound of formula: ##STR163##

or one of its salts, or each one of its pure enantiomeric forms or in racemic mixture or in variable composition.

10. A compound of formula: ##STR164##

or one of its salts, or each one of its pure enantiomeric forms or in racemic mixture or in variable composition.
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