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US08207358B2 Methods for the preparation of taxanes using chiral auxiliaries 有权
使用手性助剂制备紫杉烷的方法

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