公开(公告)号：US06603015B2

公开(公告)日：2003-08-05

申请号：US10014754

申请日：2001-12-11

申请人： Gunda I. Georg ,  Sajiv K. Nair ,  Emily Reiff ,  Ashok Rao Tunoori

发明人： Gunda I. Georg ,  Sajiv K. Nair ,  Emily Reiff ,  Ashok Rao Tunoori

IPC分类号： C07D27722

CPC分类号： C07D417/06 ,  C07B2200/07 ,  C07C45/29 ,  C07C67/31 ,  C07C67/343 ,  C07D277/24 ,  C07D493/04 ,  C07F7/1892 ,  C07C47/21 ,  C07C69/734 ,  C07C69/675

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 A and C precursors. Segment C precursors are prepared using starting nitriles, which can alternately be oxidized to ketones and converted, or reacted to form the diol with subsequent conversion to the segment. Segment A precursors are prepared by reacting a starting enone with a chiral catalyst to give an intermediate alcohol in high enantomeric excess, followed by conversion of the alcohol to the desired Segment A precursor.

公开(公告)号：US06457303B1

公开(公告)日：2002-10-01

申请号：US09798196

申请日：2001-03-02

申请人： Gunda I Georg ,  Sajiv K. Nair ,  Emily Reiff ,  Ashok Rao Tunoori ,  John T. Henri

发明人： Gunda I Georg ,  Sajiv K. Nair ,  Emily Reiff ,  Ashok Rao Tunoori ,  John T. Henri

IPC分类号： C07F708

CPC分类号： C07D417/06 ,  C07B2200/07 ,  C07C45/29 ,  C07C67/31 ,  C07D277/24 ,  C07D493/04 ,  C07F7/1892 ,  C07C47/21 ,  C07C69/734

摘要： Various epothilone precursors needed for the preparation of final epothilones are provided.

摘要翻译： 提供了制备最终埃坡霉素所需的各种埃坡霉素前体

公开(公告)号：US06211412B1

公开(公告)日：2001-04-03

申请号：US09280207

申请日：1999-03-29

申请人： Gunda I. Georg ,  Sajiv K. Nair ,  Emily Reiff ,  Ashok Rao Tunoori ,  John T. Henri

发明人： Gunda I. Georg ,  Sajiv K. Nair ,  Emily Reiff ,  Ashok Rao Tunoori ,  John T. Henri

IPC分类号： C07C4541

CPC分类号： C07D417/06 ,  C07B2200/07 ,  C07C45/29 ,  C07C67/31 ,  C07D277/24 ,  C07D493/04 ,  C07F7/1892 ,  C07C47/21 ,  C07C69/734

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.

摘要翻译： 提供了用于合成制备最终埃坡霉素所需的各种埃坡霉素前体的商业上可行的方法，包括使用立体选择性Noyori型还原合成埃坡霉素片段C的技术，以及使用醛醇缩合反应偶联埃坡霉素片段B和C. 合成方法可用于制备天然存在的片段以及大量相关的类似物及其同系物。 根据本发明的最终埃坡霉素也可以是天然存在的品种（16-元大环内酯），而其同系物和类似物优选为至多20-元大环内酯。