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Enantioselective total syntheses of belactosin A, belactosin C, and its homoanalogue
Authors:Larionov Oleg V  de Meijere Armin
Affiliation:Institut für Organische und Biomolekulare Chemie der Georg-August-Universit?t G?ttingen, Tammannstrasse 2, D-37077 Goettingen, Germany.
Abstract:[reaction: see text] Enantioselective total syntheses of belactosin A, belactosin C, and its homoanalogue have been accomplished in high overall yields (32% for belactosin A from the amino acid 10, and 35 and 36% for belactosin C and its homoanalogue, respectively). This concise approach comprises a novel sequential acylation/beta-lactonization reaction and allows a facile alteration of the substituents, thus providing a flexible route to a new family of highly active belactosin-based proteasome inhibitors.
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