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An Efficient Fmoc-SPPS Approach for the Generation of Thioester Peptide Precursors for Use in Native Chemical Ligation

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  • This work was supported by the NIH GM059380 (P.E.D.) and the Spanish Ministerio de Educación y Ciencia and the Fulbright Scholar Program (J.B.B-C).

Abstract

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Intramolecular activation of C-terminal peptides: Mildly activated N-acylurea peptides are readily formed on the solid support following chain assembly, avoiding over-activation of the C-terminus. The utility of these peptides is demonstrated by the native chemical ligation of unprotected peptides (see scheme; R=amino acid side chain).

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