New methods for the preparation of taxanes using chiral auxiliaries

摘要

The present invention relates to a stereoselective synthesis of novel ²-lactam dimers as useful precursors for the preparation of paclitaxel, docetaxel, and analogues thereof. More particularly, the new ²-lactams are prepared from readily available and enantiomerically pure chiral auxiliaries. The ²-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.