Galonić Danica P, van der Donk Wilfred A, Gin David Y
Department of Chemistry, University of Illinois, Urbana, IL 61801, USA.
J Am Chem Soc. 2004 Oct 13;126(40):12712-3. doi: 10.1021/ja046793x.
The synthesis and convergent site-selective conjugation of aziridine-2-carboxylic acid-containing peptides with thiols, both in solution and on solid support, are described. The synthesis and use of FmocAzyOH in this capacity demonstrate both the efficient incorporation and tolerance of the Azy moiety in multistep Fmoc solid-phase peptide synthesis (SPPS), as well as the competence of solution and on-bead ligation through a highly regioselective base-promoted aziridine ring-opening process.
本文描述了含氮杂环丙烷-2-羧酸的肽与硫醇在溶液中和固相载体上的合成及收敛性位点选择性共轭。FmocAzyOH在此方面的合成及应用表明，氮杂环丙烷部分在多步Fmoc固相肽合成（SPPS）中具有高效掺入性和耐受性，并且通过高度区域选择性的碱促进氮杂环丙烷开环过程，能够进行溶液和珠上连接。
