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A Study on the Synthesis of Risedronic Acid: The Role of an Ionic Liquid Additive

[ Vol. 16 , Issue. 3 ]

Author(s):

Dávid Illés Nagy, Alajos Grün, Júlia Sinkovicz, Sándor Garadnay, István Greiner and György Keglevich*   Pages 238 - 244 ( 7 )

Abstract:


Background: The synthesis of high value risedronic acid is not fully resolved, as, for the time being, the best method based on the preparation from 3-pyridylcarboxylic acid by reaction with phosphorus trichloride in methanesulfonic acid gives risedronic acid in a good yield, but in an unpure form.

Methods: Alternative protocols realizing the synthesis in sulfolane as the solvent and/or in the presence of suitable IL additive were developed to obtain the target dronic acid in a pure form.

Results & Conclusion: Using phosphorus trichloride and phosphorous acid in two equivalents quantities together with 0.6 equivalents of [bmim][BF4] without any solvent, the method afforded the target dronic acid in a yield of 66% in a pure form.

Keywords:

Risedronic acid, 3-pyridylacetic acid, P-reagents, sulfolane, ionic liquid additive, optimization.

Affiliation:

Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, 1521 Budapest, Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, 1521 Budapest, Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, 1521 Budapest, Gedeon Richter Plc., 1475 Budapest, Gedeon Richter Plc., 1475 Budapest, Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, 1521 Budapest

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