Efficient Sequential Segment Coupling Using N-Alkylcysteine-Assisted Thioesterification for Glycopeptide Dendrimer Synthesis.

[摘要]：A highly pure MUC1-derived glycopeptide dendrimer of 22 kDa was prepd. by a sequential segment coupling, achieved by an N-alkylcysteine (NAC)-assisted thioesterification. The glycopeptide having C-terminal NAC was prepd. by the Fmoc method and converted to the thioester by 3-mercaptopropionic acid treatment. The thioester was condensed with a lysine trimer carrying NAC to afford tetramer, which was then converted to the thioester. Two tetramers were condensed with ethylenediamine to give the octameric glycopeptide dendrimer.

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