Ligands for Click Chemistry

Tris[(1-benzyl-1H-1,2,3-triazol-4-yl)methyl]amine (1) and tris(2-benzimidazolylmethyl)amine (2) are extremely useful ligands for click chemistry (Hüisgen 1,3-dipolar cycloaddition reaction). In the Hüisgen reaction, copper catalysts are generally required for reaction acceleration. Sharpless and Fokin et al. have reported that 1 has a powerful binding ability to copper(I), thereby enhancing its catalytic activity. ¹⁾

Especially, Finn et al. have reported that when using 2, the reaction effectively proceeds even under lower catalyst loading conditions.²⁾