微管溶素D的全合成。
The total synthesis of tubulysin D.
作者信息
Peltier Hillary M, McMahon Jeffrey P, Patterson Andrew W, Ellman Jonathan A
机构信息
Department of Chemistry, University of California, Berkeley, California 94720, USA.
出版信息
J Am Chem Soc. 2006 Dec 20;128(50):16018-9. doi: 10.1021/ja067177z.
The first total synthesis of tubulysin D is reported. The development and application of new tert-butanesulfinamide methods allowed for rapid syntheses of the tubuvaline and tubuphenylalanine fragments. Most significantly, a route was devised and implemented to introduce and carry forward the highly labile N,O-acetal functionality. Tubulysin D is the most active member of the tubulysin family, and the efficient synthetic route described herein will allow for the rapid syntheses of analogues to probe the biological activity of this important class of natural products.
据报道，首次完成了微管溶素D的全合成。新型叔丁基亚磺酰胺方法的开发与应用使得微管缬氨酸和微管苯丙氨酸片段能够快速合成。最为重要的是，设计并实施了一条引入和推进高度不稳定的N,O - 缩醛官能团的路线。微管溶素D是微管溶素家族中活性最强的成员，本文所述的高效合成路线将能够快速合成类似物，以探究这类重要天然产物的生物活性。
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