Efficient Synthesis of Benzidronate Applying of Phosphorus Trichloride and Phosphorous Acid

Title:Efficient Synthesis of Benzidronate Applying of Phosphorus Trichloride and Phosphorous Acid

Volume: 12 Issue: 1

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

Affiliation:

Keywords: Benzidronate, intermediates, optimization, phosphorous acid, phosphorus trichloride.

Abstract: The optimized synthesis of benzidronate involves the reaction of phenylacetic acid with 3 equivalents of phosphorus trichloride and 1 equivalent of phosphorous acid in methanesulfonic acid at 85 °C followed by hydrolysis, pH adjustment and purifications. The positive effect of phosphorous acid on the yield is a novel observation and is probably limited to this model. The heap of our experimental data obtained by varying the molar equivalent quantities of the P-reagents (PCl₃ and P(OH)₃) and reacting also phenylacetic chloride and ethyl phenylacetate allowed us to draw conclusions on the possible intermediates.

Cite this article as:

Grun Alajos, Kovacs Rita, Nagy Illes David, Garadnay Sandor, Greiner Istvan and Keglevich Gyorgy, Efficient Synthesis of Benzidronate Applying of Phosphorus Trichloride and Phosphorous Acid, Letters in Drug Design & Discovery 2015; 12 (1) . https://dx.doi.org/10.2174/1570180811666141001004732

DOI https://dx.doi.org/10.2174/1570180811666141001004732	Print ISSN 1570-1808
Publisher Name Bentham Science Publisher	Online ISSN 1875-628X