Triazene as a powerful tool for solid-phase derivatization of phenylalanine containing peptides: zygosporamide analogues as a proof of concept

A novel method for the synthesis of para-substituted phenylalanine containing cyclic peptides is described. The main features of this strategy are the coupling of phenylalanine to the solid support through its side chain via a triazene linkage, on-resin cyclization of the peptide chain, cleavage of...

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Detalles Bibliográficos
Autores: Torres-García, Carolina, Pulido, Daniel, Albericio, Fernando, Royo, Miriam, Nicolás, Ernesto
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2014
País:España
Institución:Consejo Superior de Investigaciones Científicas (CSIC)
Repositorio:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/345461
Acceso en línea:http://hdl.handle.net/10261/345461
https://api.elsevier.com/content/abstract/scopus_id/84916227648
Access Level:acceso abierto
Palabra clave:Synthesis
Peptides
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Descripción
Sumario:A novel method for the synthesis of para-substituted phenylalanine containing cyclic peptides is described. The main features of this strategy are the coupling of phenylalanine to the solid support through its side chain via a triazene linkage, on-resin cyclization of the peptide chain, cleavage of the cyclic peptide from the resin under mild acidic conditions and further transformation of the resulting diazonium salt. The usefulness of this approach is exemplified by the solid-phase synthesis of some derivatives of the naturally occurring cyclic depsipeptide zygosporamide.