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The new solvates of docetaxel and C2-C3 alkyl esters of formic acid and their use for API’s preparation.

Witold S. Cieśliński 

IFOTAM Co. Ltd (IFOTAM), Andrzejewskiej 3, Łódź 92-550, Poland


The new solvates of docetaxel with  C2-C3 alkyl esters of formic acid were identified and fully characterized by methods routinely used in  the psudopolymorphs studies, such as: Termogravimetric Analysis (TGA), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FT-IR), X-Ray Powder Diffraction (XRPD). Their crystalline structures were fully confirmed by single crystal X-ray diffraction’s studies.

Figure. Crystalline structure of solvate of docetaxel and ethyl formate based on results of x-ray diffraction structural studies of single crystal.

Thus, obtained crystalline solvates of docetaxel, which chromatographic purity is not less than 99% (determined by HPLC), could be used to prepare pharmaceutical docetaxel as an anhydrous or a hydrate form, ie. trihydrate.

The known methods of purification of docetaxel are time- and labour-consuming. Generally, the purification methods of docetaxel are chromatographic methods and require usage of large amounts of solvents or multiple refining or crystallizations,  decreasing the total yields. These problems could be avoided by purification of docetaxel via solvates with  C2-C3 alkyl esters of formic acid, which are new entities, previously not described in the literature. The desolvation process of solvating solvent - ethyl formate, propyl formate or isopropyl formate, could be accomplished by any known  crystallization of docetaxel in accordance to crystallization of the anhydrous or the hydrate, especially the trihydrate.


The new solvates of docetaxel and C2-C3 alkyl esters of formic acid, their method of preparation and their use  are subject of Polish Patent application no. P-388144. PCT application is also pending.


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Presentation: Poster at VII Multidyscyplinarna Konferencja Nauki o Leku, by Witold S. Cieśliński
See On-line Journal of VII Multidyscyplinarna Konferencja Nauki o Leku

Submitted: 2010-04-19 14:35
Revised:   2010-04-21 14:15