The use of CH2Cl2 as a co-solvent with H2O in the copper (I)-catalyzed 1, 3-dipolar cycloaddition of organic azides and alkynes increased reaction rates and provided the corresponding 1, 2, 3-triazoles in excellent yields compared to other organic co-solvent systems. Moreover, we applied this discovery to prepare the functional multivalent compound in an excellent yield.