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A very efficient and convenient route for synthesis of imidazol-1-yl-acetic acid: the most important precursor for the synthesis of zoledronic acid
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1  Department of Chemistry, Science and Research Branch, Islamic Azad University, Tehran, Iran


Bisphosphonic acids are beneficial antihypercalcemic medicines and could be utilized as remedial factors for the therapy of illnesses which are specified by unusual calcium metabolism.[1] They have showed efficiency in detention bone decline and restituing normocalcemia in patients with metastatic bone disease, hypercalcemia of malignancy, osteoporosis and Paget’s disease and they have the potential for other medical usages as well. In this paper a convenient synthesis of imidazol-1-yl-acetic acid is described. Condensation reaction of a benzyl alcohol and a chloroacetyl chloride in the presence of N,N-diisopropylethylamine gave a benzyl 2-chloroacetate, which on treatment with an imidazole and then a hydrochloric acid afforded the imidazol-1-yl-acetic acid in good yield.

Keywords: Imidazol-1-yl-acetic acid, zoledronic acid, biphosphonic acids, hypercalcemia, drug precursors