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Synfacts 2007(3): 0235-0235  
DOI: 10.1055/s-2007-968188
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Synthesis of Tubulysin U

Contributor(s): Philip Kocienski
A. Dömling*, B. Beck, U. Eichelberger, S. Sakamuri, S. Menon, Q.-Z. Chen, Y. Lu, L. A. Wessjohann*
R&D Biopharmaceuticals, Martinsried and Leibniz-Institut für Pflanzenbiochemie, Halle, Germany
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Publikationsdatum:
20. Februar 2007 (online)

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Significance

The tubulysins are the most active tubulin-modifying agents known and are candidates for antibody conjugates. Three of the four amino acid components are non-proteinaceous. A key step in the synthesis depicted is the three-component coupling involving the Schöllkopf isonitrile E used to generate the thiazole ring in tubuvaline F.