Societe D'etude Et De Recherche En Ingenierie Pharmaceutique Seripharm

Novasep

Antoine Leze

Jean-Pierre Robin

Robert Dhal

Bruno Chauveau

Sonia Le Guen

Luc Chanteloup

Arnaud Lamy

Christine Corbin

Christina Corbin

The present invention generally relates to at least one precursor compound and derivatives thereof, a process for preparing a taxane, and a baccatin derivative.

Intermediates for the hemisynthesis of taxanes and preparation processes therefor

The present invention relates to novel intermediates for the hemisynthesis of taxanes and to their processes of preparation. The compounds of the present invention include precursor compounds of taxane side chains.

The present invention relates to new intermediates for the semisynthesis of taxanes and their preparation processes. It relates to derivatives of oxazolidines or oxazolidinones, as well as to new derivatives of baccatine III. The general process for the synthesis of taxanes according to the invention enables to obtain a product such as PACLITAXEL in only five steps from products available in the market, compared to nine steps in general, for processes of the prior art.

Intermediary compounds for the hemisynthesis of taxanes and preparation processes therefor

New processes for the selective protection of the 7-position of 7,10-dihydroxytaxane derivatives, using &bgr;-substituted-alkoxycarbonyl groups which are more hindered than 2,2,2-trichloroethoxycarbonyl, and which are capable of being removed by a &bgr;-elimination mechanism, and the new intermediates resulting from these processes. The new intermediates of the invention are useful for preparing taxol and analogs thereof.

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Le Mans, France

Antoine Leze