Simple, efficient one-pot method for synthesis of novel N-attached 1,2,3-triazole containing bisphosphonates.

Abstract: A practical and efficient one-pot method for synthesis of a novel kind of N-attached 1,2,3-triazole-containing bisphosphonates was developed. Michael addition reaction of sodium azide with ethylidene bisphosphonates and 1,3-dipolar click cycloaddition were reasonably integrated into one-pot reaction in the presence of sonication. Vinylidene bisphosphonate, NaN3, and terminal alkyne were employed as the reactants, CuSO4·5H2O sodium ascorbate was employed as the catalyst system, and AcOH/H2O (1:1 v/v) were employed as the solvent system to create an acidic environment to achieve optimal efficiency. [Copyright &y& Elsevier]