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Rapid Microwave-Assisted Solid-Phase Glycopeptide Synthesis

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journal contribution
posted on 2005-03-03, 00:00 authored by Takahiko Matsushita, Hiroshi Hinou, Masaki Kurogochi, Hiroki Shimizu, Shin-Ichiro Nishimura
Coupling of glycosylated Fmoc-Thr or Fmoc-Ser with N-terminal amino acids on a resin proceeded smoothly under microwave irradiation for 20 min with much higher efficiency (98% yield per coupling) than found in more general conditions. Compared with a conventional protocol, the present method greatly reduces the time required for solid-phase glycopeptide synthesis from 4 days to 7 h, as is the case with the synthesis of Muc-1-related 20-residue glycopeptide carrying five core-2 trisaccharide chains.