Process for the preparation of...

C - Chemistry – Metallurgy – 07 – D

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C07D 313/00 (2006.01) B01J 23/46 (2006.01) C07D 417/06 (2006.01)

Patent

CA 2604257

The invention comprises a novel process for the preparation of an epothilone derivative of the formula (I), wherein R1 and R2 independently from each other are hydrogen or protecting groups and R3 is methyl or trifluoromethyl, which are useful precursors in the synthesis of the desoxyepothilone derivatives of the formula (IV), wherein R is methyl or trifluoromethyl. Desoxepothilones of formula (IV) inhibit the growth of tumor cells and are therefore promising candidates for novel anticancer agents.

L'invention concerne un procédé de préparation d'un dérivé d'épothilone de formule (I), dans laquelle R1 et R2 représentent de manière indépendante l'hydrogène ou des groupes protecteurs et R3 désigne un méthyle ou trifluorométhyle, utile comme précurseur dans la synthèse des dérivés de la désoxyépothilone de formule (IV), R représentant un méthyle ou trifluorométhyle. Des désoxépothilones de formule (IV) inhibent la croissance de cellules tumorales et constituent, par conséquent, des candidats prometteurs pour des agents anti-cancer.

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