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Efficient syntheses of zoledronic acid as an active ingredient of a drug against osteoporosis

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posted on 2018-02-13, 16:43 authored by Dávid Illés Nagy, Alajos Grün, Krisztina Lévay, Sándor Garadnay, István Greiner, György Keglevich

The reaction of 1H-imidazol-1-ylacetic acid and two equivalents of phosphorus trichloride/phosphorous acid at 75 °C in sulfolane, or in the presence of catalytic amounts of [bmim][BF4] afforded zoledronic acid in yields up to 75%. The joint use of the ionic liquid additive and sulfolane as the solvent was synergetic affording highly valuable zoledronic acid in a record yield of 93%.

Funding

The research was supported by Gedeon Richter Plc and by the National Research Development and Innovation Office (K119202).

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