Rapid synthesis of acyl transfer auxiliaries for cysteine-free native glycopeptide ligation

Rapid synthesis of acyl transfer auxiliaries for cysteine-free native glycopeptide ligation
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DOI:
10.1021/ol048145o
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发表时间:
2004-12-09
期刊:
影响因子:
5.2
通讯作者:
Anderson, DW
Anderson, DW
中科院分区:
化学1区
文献类型:
--
作者:
Macmillan, D;Anderson, DW

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描述了用于无半胱氨酸的天然化学连接的TFA-可裂解的4,5,6-三甲氧基-2-巯基苄基和1-(2,4-二甲氧基苯基)-2-巯基乙基类助剂的快速、简便的路线。快速合成,加上温和的切割条件无疑将扩大这些助剂的效用,特别是在化学上脆弱的肽修饰,如糖基化存在。
Rapid, facile routes to the TFA-cleavable 4,5,6-trimethoxy-2-mercaptobenzyl and 1-(2,4-dimethoxyphenyl)-2-mercaptoethyl classes of auxiliaries for cysteine-free native chemical ligation are described. Rapid synthesis, coupled with mild cleavage conditions will undoubtedly broaden the utility of such auxiliaries, particularly where chemically fragile peptide modifications such as glycosylation are present.