Synthesis of Macrocycles and Click Chemistry

Click chemistry reactions are gaining increasing importance in the synthetic construction of complex nanoscale architectures. The Cu(I)-catalyzed azide–alkyne cycloaddition (CuAAC) and the thiol–ene reaction are established click chemistry methodologies. Given their efficiencies, they have been widely applied for bioconjugation, polymer, and dendrimer synthesis. More recently, they have been utilized for the efficient formation of rigid or shape-persistent, preorganized macrocyclic species. This strategy also allows the installment of useful functionalities, such as thioethers, or polar and function-rich 1,2,3-triazole moieties, directly embedded in the macrocyclic structure. This chapter analyzes the state of the art in this context and provides some elements of perspective for future applications.