Ex Post Glycoconjugation of Phthalocyanines

For the first time, fully fledged phthalocyanines (Pcs) were ex post glycoconjugated, that is, via 1,3-dipolar cycloaddition reaction. This divergent approach gains rapid access to a broad range of highly diverse Pcs bearing chemically sensitive substituents. This will be a breakthrough in generating structure−activity relationships (SAR) for the development of novel bioactive molecules.

本研究首次实现了结构完备的酞菁（phthalocyanines, Pcs）的后置糖缀合修饰，即通过1,3-偶极环加成反应（1,3-dipolar cycloaddition reaction）完成该过程。该发散式合成策略可快速获得一系列带有化学敏感取代基的高度多样化酞菁化合物，这将为构建构效关系（structure−activity relationships, SAR）以开发新型生物活性分子带来突破性进展。