CommunicationDevelopment of aspartic acid ligation for peptide cyclization derived from serine/threonine ligation

Add time:09/26/2019    Source:sciencedirect.com

Based on a mechanism analogous to the serine/threonine ligation, the aspartic acid ligation, which is facilitated by the γ-amino alcohol based ligation and oxidation, is developed and applied to the synthesis of cyclic peptides. The γ-hydroxyl group triggers the ring-chain tautomerization via a 6-endo-trig process, while the δ-hydroxyl group facilitates the oxidative cleavage of the vicinal diol to give carboxylic acid.

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