Synthesis of epothilones
申请(专利)号:
US19990280207
申请日期:
1999-03-29
公开/公告号:
US6211412B1
公开/公告日期:
2001-04-03
申请(专利权)人:
THE UNIVERSITY OF KANSAS
被引量:
摘要:
Commercially feasible methods for synthesizing various epothilones precursors needed for the preparation of final epothilones are provided, including techniques for the synthesis of epothilone segment C using a stereoselective Noyori-type reduction, and the coupling of epothilone segments B and C using an aldol condensation reaction. The synthesis methods may be used to prepare naturally occurring segments as well as a large number of related analogs and homologs thereof. Final epothilones in accordance with the invention may also be of the naturally occurring variety (16-membered macrolides), while the homologs and analogs thereof are preferably up to 20-membered macrolides.
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