Wessjohann Ludger A, Rivera Daniel G, León Fredy
Department of Bioorganic Chemistry, Leibniz Institute of Plant Biochemistry, Weinberg 3, Halle/Saale, Germany.
Org Lett. 2007 Nov 8;9(23):4733-6. doi: 10.1021/ol7021033. Epub 2007 Oct 9.
A novel approach to freeze the imine exchange process in dynamic combinatorial libraries by Ugi reactions was developed. Macrocyclic oligoimine libraries previously formed and altered by addition of metal templates are efficiently quenched by multiple multicomponent reactions. The approach may be considered as an alternative to the typical reduction with borohydrides and delivers polyazamacrocycles with variable side arms. High dilution is not required to achieve high yields.
开发了一种通过乌吉反应冻结动态组合库中亚胺交换过程的新方法。先前通过添加金属模板形成并改变的大环低聚亚胺库可通过多个多组分反应有效淬灭。该方法可被视为用硼氢化物进行典型还原的替代方法,并能提供具有可变侧链的聚氮杂大环化合物。实现高产率不需要高稀释度。