Total synthesis of tubulysin U and V

被引:98
作者
Doemling, Alexander
Beck, Barbara
Eichelberger, Uwe
Sakamuri, Sukumar
Menon, Sanjay
Chen, Quin-Zene
Lu, Yingchun
Wessjohann, Ludger A.
机构
[1] R& Biopharmaceutu GmbH, D-82152 Martinsried, Germany
[2] Leibniz Inst Pflanzenbiochem, Abt Nat & Wirkstoffchem, D-06120 Halle, Germany
[3] Morphochem Inc, Monmouth Jct, NJ 08852 USA
关键词
antitumor agents; multicomponent reactions; natural products; peptide coupling; thiazoles;
D O I
10.1002/anie.200601259
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Multicomponent method: Tubulysins are among the most potent cytotoxic agents known. Now the first total synthesis of some members has been achieved by utilizing a rapid three-component reaction for the synthesis of the unusual central thiazole amino acid tubuvaline (see scheme; Boc = tert-butoxycarbonyl, Ac = acetyl), thereby opening new perspectives for anticancer drug development. (Chemical Equation Presented). © 2006 Wiley-VCH Verlag GmbH & Co. KGaA.
引用
收藏
页码:7235 / 7239
页数:5
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