Abstract An efficient synthesis of novel mono and bis-1, 2, 3-triazoles 3′-azido-2′- deoxythymidine (AZT) derivatives via copper (I)-catalyzed 1, 3-dipolar cycloaddition reaction is described. Starting from AZT and terminal alkyne derivatives, mono and bis-1, 2, 3-triazole AZT derivatives are regioselectively obtained in good yields under mild conditions using CuSO4· 5H2O and sodium ascorbate as a catalyst system, and t-BuOH/H 2 O (1: 1, v/v) as ...