Department of Chemistry, Technical University of Denmark, DK-2800 Kgs. Lyngby, Denmark.
Org Lett. 2010 Dec 3;12(23):5414-7. doi: 10.1021/ol102209p. Epub 2010 Nov 4.
A broadly useful acid-labile traceless azido linker for the solid-phase synthesis of NH-1,2,3-triazoles is presented. A variety of alkynes were efficiently immobilized on a range of polymeric supports by Cu(I)-mediated azide-alkyne cycloadditions. Supported triazoles showed excellent compatibility with subsequent peptide chemistry. Release of pure material (typically >95%) from the solid support was readily achieved by treatment with aqueous TFA.
本文介绍了一种广泛适用于 NH-1,2,3-三唑固相合成的酸不稳定无痕迹叠氮化物连接剂。通过铜（I）介导的叠氮化物-炔烃环加成反应，各种炔烃被有效地固定在一系列聚合物载体上。负载的三唑与随后的肽化学具有优异的相容性。通过用三氟乙酸（TFA）水溶液处理，可从固体载体上轻易地获得纯物质（通常>95%）的释放。
