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•The O-Boc-protected glycosylated amino acids were easily prepared.•These building blocks can be applied to synthesize both N- and O-glycopeptides.•The use of these compounds can avoid side reactions in glycopeptide synthesis.
Development of a synthetic method for the preparation of homogeneous glycopeptides and glycoproteins is important for the elucidation of their structures and functions. Here, we report on the concise and facile synthesis of glycopeptides using Boc groups for the protection of carbohydrate hydroxyl groups. This method enables us to remove the protecting groups from peptide and carbohydrate moieties in a single-step process without undesirable any side reaction.