Di-CuAAC of di-alkynes 5b–7b with benzyl azide derivatives 1a–4a in water in the presence of RG^a,b.

^aReaction condition: di-alkyne derivative (1 mmol) and azides (2.1 mmol), Cu(ii) (1 mol%), Na-l-ascorbate (3 mol%), RG (1 mol%), water (10 mL), 45 min, 80 °C.

^bIsolated yields.