The present invention relates to dendrimers being multivalently substituted with active groups, as well as to processes for the preparation thereof and to the use of such multivalent dendrimers.
The active compounds encompass peptides, including oligopeptides up to entire proteins, carbohydrates and pharmaceutically active drug molecules.
Active compounds are chemoselectively bound to the dendrimer periphery using a cycloaddition reaction (also termed as "click" reaction) between an alkyne group and either an azide or a nitrile oxide, leading to a 1,4-disubstituted 1,2,3-triazole or a 1,4-disubstituted 1,2-oxazole bridging unit. Such reaction is catalyzed by Cu(I) compounds. Microwave irradiation improves the efficiency of the click reaction.
本发明涉及被多价活性基团取代的树枝状聚合物,以及其制备方法和这种多价
树脂的用途。活性化合物包括肽,包括寡肽直至整个蛋白质,
碳水化合物和药用活性药物分子。活性化合物通过环加成反应(也称为“点击”反应)与
树脂周围的树枝状聚合物具有
化学选择性地结合,其中环加成反应是通过炔基与偶氮基或亚硝基氧化物之间的反应实现的,从而形成1,4-二取代的
1,2,3-三唑或1,4-二取代的1,2-
噁唑桥联单元。这种反应由Cu(I)化合物催化。微波辐射提高了点击反应的效率。