Journal
SYNLETT
Volume 31, Issue 5, Pages 507-511Publisher
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0039-1691572
Keywords
benzyne; aryne; dehydroalanine; alpha,alpha-disubstituted benzocyclobutane amino acids; peptidomimetic
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A mild and general method for the synthesis of alpha,alpha-disubstituted benzocyclobutane amino acids through a [2+2] annulation of benzyne with dehydroalanine is described. Yields up to 88% of the constrained quaternary amino acids can be obtained and its application in peptidomimetic synthesis is demonstrated.
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