Development of a L‐Tryptophan‐Based Ligand for Regioselective Copper Catalyzed N ² ‐Arylation of 1,2,3‐Triazoles

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Abstract 2‐aryl‐1,2,3‐triazoles are important compounds that find applications in Medicinal chemistry, diagnostics, catalysis and others. However, only few methodologies for their preparation is found in the literature. The development of a post cycloaddition N 2 selective arylation towards these compounds would benefit from a more convergent strategy. In the present communication, the development of a new tryptophan‐based ligand allowed the selective arylation of the N 2 ‐position of 1,2,3‐triazoles using recyclable CuFe 2 O 4 nanoparticles. This method was efficient in furnishing N 2 ‐arylated and heteroarylated 1,2,3‐triazoles in good yields and excellent N 2 ‐selectivity. The methodology developed found application in the synthesis of the 2‐aryl‐1,2,3‐triazoyl fragment of the drug suvorexant (Belsomra®).