Total synthesis of tubulysins U and V

被引:71
作者
Sani, Monica
Fossati, Giacomo
Huguenot, Florent
Zanda, Matteo
机构
[1] Politecn Milan, CNR, Ist chim Riconoscimento Mol, I-20131 Milan, Italy
[2] Politecn Milan, Dipartimento CMIC, I-20131 Milan, Italy
关键词
antitumor agents; enantioselectivity; natural products; peptide coupling; total synthesis;
D O I
10.1002/anie.200604557
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Meeting the challenge: A reliable and modular reaction sequence has been developed for the synthesis of the challenging tubulysin framework. This route allows preparation of hundreds of milligrams of the stereochemically pure tetrapeptides (see picture), which are produced in small amounts by two different species of myxobacteria. Thus, full biological evaluation of the tubulysins and their analogues is now a real possibility. (Chemical Equation Presented). © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码:3526 / 3529
页数:4
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