Rapid access to Asp/Glu sidechain hydrazides as thioester precursors for peptide cyclization and glycosylation.
2021
Head-to-sidechain macrocylic peptides, and neoglycopeptides, were readily prepared by site-specific amidation of aspartic and glutamic acid sidechain hydrazides. Hydrazides, serving as latent thioesters, were introduced through regioselective opening of the corresponding Nα-Fmoc protected anhydride precursors.
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