Facile production of mono-substituted urea side chains in solid phase peptide synthesis
Facile production of mono-substituted urea side chains in solid phase peptide synthesis
复制标题
DOI：
10.1002/bip.20737
复制
发表时间：
2007-07-01
期刊：
影响因子：
2.9
通讯作者：
Kennan, Alan J.
中科院分区：
文献类型：
--
作者：
Diss, Maria L.;Kennan, Alan J.
报道了一种在Boc固相肽合成过程中直接生成含脲肽的方法。伯胺侧链通过中间体氨基甲酸对硝基苯基酯在两个步骤中转化为单烷基脲。使用对甲氧基苄基胺作为氨等价物由标准树脂裂解方法提供单烷基最终产物，而不需要额外的步骤。该反应是高效的，并且适用于可变长度的侧链和肽。(c)2007 Wiley Periodicals，Inc.
A method is reported for the straightforward generation of urea-containing peptides during Boc solid phase peptide synthesis. Primary amine side chains are converted to mono-alkyl ureas in two steps via an intermediate p-nitrophenyl carbamate. Use of p-methoxybenzyl amine as an ammonia equivalent affords mono-alkyl final products from standard resin cleavage methods, without the need for additional steps. The reaction is highly efficient and applicable to variable length side chains and peptides. (c) 2007 Wiley Periodicals, Inc.