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- Title
A One-Pot and Efficient Synthesis of Zoledronic Acid Starting from Tert-butyl Imidazol-1-yl Acetate.
- Authors
Ratrout, Samer; Al Sarabi, Ala'eddine; Sweidan, Kamal
- Abstract
A one-pot synthesis of zoledronic acid in high yield is described. The procedure involves a non-aqueous ester cleavage of the tert-butyl imidazol-1-yl acetate under dry conditions in the presence of methanesulfonic acid as solubilizer and chlorobenzene as solvent to afford in situ the corresponding imidazolium methanesulfonate salt which yields zoledronic acid upon reaction with phosphoric acid and phosphorus oxychloride. A possible chemical mechanism for the synthesis of this acid is described.
- Subjects
ZOLEDRONIC acid; IMIDAZOLES; AQUEOUS solutions; METHANESULFONATES; PHOSPHORUS oxychloride
- Publication
Pharmaceutical Chemistry Journal, 2015, Vol 48, Issue 12, p835
- ISSN
0091-150X
- Publication type
Article
- DOI
10.1007/s11094-015-1205-0