The synthesis of risedronic acid and alendronate from 3-pyridylacetic acid and γ- aminobutyric acid, respectively, using phosphorus oxychloride and phosphorous acid as the P-reagents and methanesulfonic acid as the solvent was optimized, and the role of phosphorus oxychloride and phosphorous acid in the reaction was clarified.
Keywords: Alendronate, mechanism, optimization, phosphorus oxychloride, phosphorous acid, risedronic acid, synthesis.