Taxane derivative crystal and method for preparing the same

Details Taxane derivative crystal and method for preparing the same Taxane derivative crystal and method for preparing the same

C - Chemistry, Metallurgy

07

D

C07D 493/04 (2006.01) A61K 31/443 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2468953

A crystal of (1S,2S,3R,4S,5R,8R,9S,10R,13S)-4-acetoxy-2-benzoyloxy--9, 10-[(1 S)-2-(dimethylamino)ethylidenedioxy]-5,20-epoxy-1-hydroxytax-11-en-13- yl (2R,3S)-3-(tert-butoxycarbonylamino)-3-(3-fluoro-2-pyridyl)-2- hydroxypropionate, which has characteristic peaks at diffraction angles (2.theta.) of 6.2°, 10.3°, 10.7°, 11.4°, and 12.0° in a powder X-ray diffraction pattern, and a method for preparing the aforementioned crystal, which comprises the step of performing crystallization by using an organic solvent selected from the group consisting of a ketone type solvent, a nitrile type solvent, and a mixture thereof, or a mixture of said organic solvent and water.

L'invention concerne des cristaux de (1S,2S,3R,4S,5R,8R,9S,10R,13S)-4-acétoxy-2-benzoyloxy-9,10-[(1S)-2-(diméthylamino)éthylidènedioxyl]-5,20-époxy-1-hydroxytax-11-èn-13-yl(2R,3S)-3-(tert-butoxycarbonylamino)-3-(3-fluoro-2-pyridyl)-2-hydroxyproprionate, présentant, dans le diagramme de diffraction aux rayons X sur poudre, des pics caractéristiques à des angles de diffraction (2.theta.) de 6,2·, 10,3·, 10,7·, 11,4· et 12,0·, ainsi qu'un procédé de production de ces cristaux consistant à mener une cristallisation au moyen d'un solvant organique sélectionné parmi le groupe comprenant des cétones, des nitriles et des mélanges des deux ou un mélange du solvant organique et d'eau.

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