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Synthetic Communications
An International Journal for Rapid Communication of Synthetic Organic Chemistry
Volume 48, 2018 - Issue 6
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Original Articles

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

, , , , &
Pages 663-671 | Received 26 Oct 2017, Published online: 13 Feb 2018
 

ABSTRACT

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%.

GRAPHICAL ABSTRACT

Additional information

Funding

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

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