Miller Nicole, Williams Geoffrey M, Brimble Margaret A
Department of Chemistry, University of Auckland, Private Bag 92019, Auckland, New Zealand.
Org Lett. 2009 Jun 4;11(11):2409-12. doi: 10.1021/ol9005536.
Microwave-enhanced click glycoconjugation of a propargylated alpha-GalNAc sugar moiety with an azido-functionalized amino acid or multiazido-functionalized peptides using a catalytic quantity of Cu(I) enabled a high-yielding and rapid synthesis of a "Tn-antigen mimic" and click analogues of antifreeze glycopeptides, thus demonstrating a valuable synthetic platform for the synthesis of biologically relevant neoglycopeptides.
使用催化量的Cu(I)，将炔丙基化的α-GalNAc糖部分与叠氮基官能化的氨基酸或多叠氮基官能化的肽进行微波增强点击糖缀合反应，能够高产率且快速地合成“Tn抗原模拟物”和抗冻糖肽的点击类似物，从而证明了该合成平台对于合成具有生物学相关性的新糖肽具有重要价值。
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