Fmoc-aza-β3-Lys-OAllyl and Fmoc-aza-β3-Asp-OAllyl for On-Resin Head-to-tail Cyclization of Aza-Β3-peptides
Tetrahedron letters(2013)
摘要
A rapid and efficient Fmoc/t-Bu solid-phase peptide synthesis (SPPS) of cyclic aza-β3-peptide analogs by allyl strategy is described. Our synthetic approach includes the synthesis of two new aza-β3-amino acids, Fmoc-aza-β3-Lys-OAllyl and Fmoc-aza-β3-Asp-OAllyl, then the resin attachment of the first aza-β3-amino acid via its side chain, successful use of combination of three orthogonal removable protecting groups, stepwise solid-phase synthesis of linear peptide analog, and on-resin head-to-tail cyclization.
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关键词
Aza-beta(3)-amino acids,Allyl protection,Lysine analog,Aspartique analog,Cyclic pseudopeptides
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