Efficient syntheses of zoledronic acid as an active ingredient of a drug against osteoporosis. Issue 6 (19th March 2018)

• Record Type: Journal Article
• Authors: Nagy, Dávid Illés; Grün, Alajos; Lévay, Krisztina; Garadnay, Sándor; Greiner, István; Keglevich, György
• Is Part Of: Synthetic communications. Volume 48:Issue 6(2018)
• Page Start: 663
• Page End: 671
• Publication Date: 2018-03-19
• Subjects: 1H-imidazol-1-ylacetic acid -- ionic liquid additive -- P-reagents -- sulfolane -- synthesis -- zoledronic acid; Organic compounds -- Synthesis -- Periodicals; Chemistry, Organic; Synthesis; 547.205
• DOI: 10.1080/00397911.2017.1410894
• Languages: English
• ISSNs: 0039-7911

Abstract

ABSTRACT: The reaction of 1 H -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: