Process for preparing taxol-type compound from beta-lactam precursors.

摘要

Taxol-type compounds are produced by coupling baccatin III-type compounds (and related alcohols) with chemoenzymatically produced beta -lactam enantiomers. The beta -lactam enantiomers are produced from racemic starting substituted beta -lactams through lipase contacting to achieve either enantioselective hydrolysis or enantioselective transesterification (the latter with an added 1-substituted ethenyl acetate). Preferred beta -lactam enantiomers are coupled to the C-13 hydroxyl of the starting baccatin III-type compounds which are derived from 10-deacetyl baccatin III. Certain of the beta -lactam enantiomers are new as are taxol-type compounds produced by the coupling reaction.