Efficient Synthesis of Benzidronate Applying of Phosphorus Trichloride and Phosphorous Acid

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

Journal Name: Letters in Drug Design & Discovery

Volume 12 , Issue 1 , 2015

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Graphical 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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Article Details

Year: 2015
Published on: 29 October, 2014
Page: [78 - 84]
Pages: 7
DOI: 10.2174/1570180811666141001004732

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PDF: 26
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