Improved solid-phase peptide synthesis method utilizing α-azide-protected amino acids

被引:183
作者
Lundquist, JT [1 ]
Pelletier, JC [1 ]
机构
[1] Wyeth Ayerst Res, Div Discovery Chem, Radnor, PA 19087 USA
关键词
D O I
10.1021/ol0155485
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
[GRAPHICS] Pure alpha -azido acids were prepared using an efficient diazo transfer method followed by buffered workup, These building blocks were used to prepare small peptides on Wang resin by two approaches, Peptides prone to diketopiperazine formation were prepared in good yields by coupling acids to resin bound iminophosphoranes during Fmoc-Wang synthesis, The iminophosphoranes can also be hydrolyzed under neutral conditions to provide unprotected amines ready for further coupling.
引用
收藏
页码:781 / 783
页数:3
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