1,2,3-Triazoles as versatile directing group for selective sp2 and sp3 C-H activation: cyclization vs substitution

Selective cyclization and substitution was achieved with designated 1,2,3-triazole acid auxiliary groups under Pd catalyzed C-H activation conditions. Both sp(2) and sp(3) C-H bonds were effectively activated, giving the desired products in good yields. This result revealed the first successful example of exclusive substitution using 1,2,3-triazole ligands, while another triazole-containing directing group dominantly gave cyclization under identical conditions.