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Synfacts 2007(3): 0235-0235
DOI: 10.1055/s-2007-968188
DOI: 10.1055/s-2007-968188
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York
Synthesis of Tubulysin U
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
Further Information
Publication History
Publication Date:
20 February 2007 (online)
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.