Efficient Continuous-Flow Synthesis of Macrocyclic Triazoles

Anne-Catherine Bédard, Jeffrey Santandrea, Shawn K. Collins

• Department of Chemistry and Centre for Green Chemistry and Catalysis, University of Montreal

The continuous-flow synthesis of a series of 11- to 26-membered macrocycles via copper-catalyzed azide-alkyne cycloaddition is reported. The approach employs homogeneous catalysis to promote formation of triazole-containing macrocycles in good to excellent yields (65–90%) at relatively high concentration (30–50 mM) using a phase separation strategy.

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