Abstract: The present invention relates to a stereoselective synthesis of novel ?-lactam dimers as useful precursors for the preparation of paclitaxel, docetaxel, and analogues thereof. More particularly, the new ?-lactams are prepared from readily available and enantiomerically pure chiral auxiliaries. The ?-lactams are then reacted with a suitably protected taxane to produce diastereomerically enriched side chain-bearing taxanes. Finally, the chiral auxiliary is cleaved and protecting groups are removed to provide the desired taxane.

Abstract: The present invention relates to a new process for the preparation of 9-dihydrobaccatin III intermediates as useful precursors for the preparation of paclitaxel, 1, docetaxel, 2, and analogues thereof. More particularly, the process comprises the steps of (i) concomitantly deacetylating esters at the 10-position and 13-position of 9-dihydro-13-acetylbaccatin III to form 9-dihydro-10-deacetylbaccatin III; (ii) protecting a hydroxy group at the 7-position of 9-dihydro-10-deacetylbaccatin III; and (iii) acylating a hydroxy group at the 10-position to form a compound of formula II.

Abstract: The invention relates to new carbohydrate derivatives of paclitaxel and docetaxel with increased solubility in water as compared to the parent compounds, paclitaxel and docetaxel These derivatives are produced from naturally occurring precursor molecules which upon hydrolysis yield these natural precursors and the original paclitaxel and docetaxel molecules. The present invention also relates to the composition and the use of such derivatives for cancer therapy. These derivatives may also be used in antifungal or antiviral therapy.