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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

[ Vol. 18 , Issue. 1 ]

Author(s):

Alajos Grün, Zsuzsanna Szalai and György Keglevich*   Pages 8 - 12 ( 5 )

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.

Affiliation:

Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, 1521 Budapest, Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, 1521 Budapest, Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, 1521 Budapest

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