Fmoc solid-phase synthesis of peptide thioesters by masking as trithioortho esters |
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Authors: | Brask Jesper Albericio Fernando Jensen Knud J |
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Institution: | Department of Chemistry, Royal Veterinary and Agricultural University, DK-1871 Frederiksberg, Denmark. |
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Abstract: | reaction: see text] Total chemical synthesis of proteins by chemoselective ligation relies on C-terminal peptide thioesters as building blocks. Their preparation by standard Fmoc solid-phase peptide synthesis is made difficult by the lability of thioesters to aminolysis by the secondary amines used for removal of the Fmoc group. Here we present a novel backbone amide linker (BAL) strategy for their synthesis in which the thioester functionality is masked as a trithioortho ester throughout the synthesis. |
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