CuAAC chemistry is used to compose incredible synthetic molecular architectures and acts as a true click chemistry reaction allowing densely functional molecular fragments to be joined in a highly controlled manner. Using supercatalysts based on our mechanistic understanding and in the absence of oxygen, CuAAC reactions are superior even in bioligation chemistry. The catalytic cycle provides an organometallic intermediate reacting through electrophilic or oxidative escape valves resulting in trisubstituted 1,2,3-triazoles and allowing CuAAC-multicomponent reactions. The ease of CuAAC provides new pathways in the development of exquisitely selective macrocyclic protein–protein interaction inhibitors (PPIs) and enzyme inhibitors as putative novel classes of pharmaceuticals.

CuAAC化学用于组成令人难以置信的合成分子结构，并充当真正的点击化学反应，使高度功能化的分子片段以高度受控的方式连接。根据我们对机理的理解并在没有氧气的情况下使用超级催化剂，即使在生物连接化学中，CuAAC反应也很出色。催化循环提供了一种有机金属中间体，该中间体通过亲电或氧化逃逸阀反应，生成三取代的1,2,3-三唑并允许CuAAC-多组分反应。CuAAC的简便性为开发精细选择性大环蛋白-蛋白相互作用抑制剂（PPI）和酶抑制剂作为推定的新型药物提供了新的途径。