title: Advanced strategies for efficient macrocyclic Cu(I)-catalyzed cycloaddition of azides.
abstract: An advanced strategy for efficient macrocyclic Cu(I)-catalyzed cycloaddition is described. The key features include employing azide-iodoalkyne cycloadditions (CuAiAC), low catalyst loadings, relatively high concentrations (30 mM → 300 mM), and application to continuous flow. The remarkably efficient new tool affords a variety of macrocyclic skeletons having either different alkyl, aryl, or amino acid spacers in high yields (70-97%). The macrocyclic CuAiAC process affords macrocycles having an iodotriazole moiety that can be further functionalized using standard Pd-catalyzed cross-couplings.
authors.affiliation: Department of Chemistry and Centre for Green Chemistry and Catalysis, Université de Montréal , CP 6128 Station Downtown, Montréal, Québec Canada , H3C 3J7.
authors.forename: Anne-Catherine
authors.initials: AC
authors.lastname: Bédard
authors.forename: Shawn K
authors.initials: SK
authors.lastname: Collins