Total Synthesis of Tubulysins U and V

Total Synthesis of Tubulysins U and V

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 di...

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Veröffentlicht in:Angewandte Chemie International Edition 2007-01, Vol.46 (19), p.3526-3529
Hauptverfasser: Sani, Monica, Fossati, Giacomo, Huguenot, Florent, Zanda, Matteo
Format: Artikel
Sprache:eng
Schlagworte:
Antineoplastic Agents - chemical synthesis
antitumor agents
Biological Products - chemical synthesis
enantioselectivity
Models, Chemical
Myxococcales - chemistry
natural products
Oligopeptides - chemical synthesis
peptide coupling
Pipecolic Acids - chemical synthesis
total synthesis
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Zusammenfassung: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.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.200604557