Matsushita Takahiko, Hinou Hiroshi, Kurogochi Masaki, Shimizu Hiroki, Nishimura Shin-Ichiro
Division of Biological Sciences, Graduate School of Science, Frontier Research Center for the Post-Genome Science and Technology, Hokkaido University, N21 W11, Sapporo 001-0021, Japan.
Org Lett. 2005 Mar 3;7(5):877-80. doi: 10.1021/ol0474352.
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. [structure: see text]
在微波辐射下，糖基化的Fmoc-苏氨酸或Fmoc-丝氨酸与树脂上的N端氨基酸的偶联反应顺利进行20分钟，效率比更常规条件下高得多（每次偶联产率98%）。与传统方法相比，本方法极大地缩短了固相糖肽合成所需的时间，从4天减至7小时，就像合成带有五条核心-2三糖链的Muc-1相关20残基糖肽的情况一样。[结构：见正文]
