Total Synthesis of Tubulysin U and V



This article is corrected by:

  1. Errata: Total Synthesis of Tubulysin U and V Volume 46, Issue 14, 2347–2348, Article first published online: 16 March 2007

  • U.E. and L.A.W. acknowledge support from the State of Saxony-Anhalt as part of a HWP grant. We thank Dr. A. Porzel for special NMR analysis and Prof. G. Höfle for providing reference spectra and preliminary activity and isolation information.


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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.