Labelled taxanes

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 305/14 (2006.01) C07F 7/18 (2006.01) G01N 33/48 (2006.01)

Patent

CA 2479273

There are provided stable labelled taxanes, characterized in that the isotopes are present in the benzoyloxy group at the C-2 position. More particularly, one or more of the hydrogen or carbon atoms of the benzoyl residue at the C-2 position of the taxane skeleton is replaced respectively from deuterium or 13C.A process for their preparation and their use as internal standard in analytical methods for determining taxanes, useful anticancer drugs, are also provided.

La présente invention a trait à des taxanes stables marqués, caractérisés en ce que les isotopes sont présents dans le groupe benzoyloxy en position C-2. Plus particulièrement, un ou des parmi les atomes d'hydrogène ou de carbone du résidu de benzoyle à la position C-2 d'un squelette de taxane est substitué respectivement par le deutérium ou ?13¿C. L'invention a trait également à un procédé pour leur préparation et leur utilisation en tant qu'étalon interne dans des procédés analytiques pour la détermination de taxanes, utiles en tant que médicaments anticancéreux.

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