High-yielding Staudinger ligation of a phosphinothioester and azide to form a peptide
High-yielding Staudinger ligation of a phosphinothioester and azide to form a peptide
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DOI：
10.1021/ol006739v
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发表时间：
2001-01-11
期刊：
影响因子：
5.2
通讯作者：
Raines, RT
中科院分区：
文献类型：
--
作者：
Nilsson, BL;Kiessling, LL;Raines, RT
施陶丁格连接可用于将具有C-末端硫代膦酯的肽与具有N-末端α-叠氮基的另一肽偶联，以形成不含残留原子的单一肽。在这里，二苯基膦基甲烷乙硫基酯显示出这种转化的高分离产率。这一发现为蛋白质的全合成提供了一种强大而通用的新方法。
[GRAPHICS]The Staudinger ligation can be used to couple a peptide with a C-terminal phosphinothioester to another with an N-terminal alpha -azido group to form a single peptide that contains no residual atoms. Here, diphenylphosphinomethanethiol thioesters are shown to give high isolated yields for this transformation. This finding provides precedent for a powerful and versatile new method for the total synthesis of proteins.