Modular Synthesis of Triazole‐Containing Triaryl α‐Helix Mimetics

We describe novel scaffold designs for nonpeptidic α‐helix mimetics. The tricyclic scaffolds contain triazoles and reproduce amino acid side chains i , i +3, and i +7. The three different scaffolds are synthetically readily accessible, allow the introduction of further substituents to increase the versatility, and are suitable for library design. A modular synthesis route using Cu I ‐ and Ru II ‐catalyzed azide–alkyne [3+2] cycloadditions as central steps was developed. To demonstrate the methodology, we have prepared a library of compounds containing all three scaffolds.