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Letters in Drug Design & Discovery

Editor-in-Chief

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

Efficient Synthesis of Benzidronate Applying of Phosphorus Trichloride and Phosphorous Acid

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

Volume 12, Issue 1, 2015

Page: [78 - 84] Pages: 7

DOI: 10.2174/1570180811666141001004732

Price: $65

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.

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

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