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Letters in Organic Chemistry

Author(s): Alajos Grün, Zsuzsanna Szalai and György Keglevich*

DOI: 10.2174/1570178617999200730203738

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“Greener” Synthesis of Zoledronic Acid from Imidazol-1-yl-acetic Acid and P-Reagents Using Diethyl Carbonate as the Solvent Component

Page: [8 - 12] Pages: 5

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Abstract

The synthesis of a third generation dronic acid, zoledronic acid by the reaction of imidazol- 1-yl-acetic acid with phosphorus trichloride/phosphorous acid in diethyl carbonate (DEC) as a “green” solvent, and in DEC – methanesulfonic acid (MSA) solvent mixtures is described. The earlier not “green” and expensive MSA and sulfolane solvents may be replaced by DEC.

Keywords: Zoledronic acid, imidazol-1-yl-acetic acid, P-reagents, diethyl carbonate, methanesulfonic acid, sulfolane.