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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

The Synthesis of Risedronic Acid and Alendronate Applying Phosphorus Oxychloride and Phosphorous Acid in Methanesulfonic Acid

Author(s): Alajos Grun, Rita Kovacs, Sandor Garadnay, Istvan Greiner and Gyorgy Keglevich

Volume 12, Issue 4, 2015

Page: [253 - 258] Pages: 6

DOI: 10.2174/1570180811666141010220427

Abstract

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.

Graphical Abstract

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