“Greener” synthesis of bisphosphonic/dronic acid derivatives

Abstract: According to literature, the synthesis of dronic acid derivatives from the corresponding carboxylic acids using phosphorus trichloride and phosphorous acid as the P-reactants is controversial, due to the wide range of molar ratios and diverse conditions. In this minireview, we summarize our results on the clarification of these problems. For example, with zoledronic acid and risedronic acid, we found that, using methanesulfonic acid (MSA) as the solvent, 3.2 equivalents of phosphorus trichloride was enough. Generalizing this optimized method, etidronate, fenidronate, ibandronate and alendronate were obtained in yields of 38%–57%, which is reasonable for valuable dronates, and in most cases, with high purities. Mechanistic aspects are also discussed.

Location
Deutsche Nationalbibliothek Frankfurt am Main
Extent
Online-Ressource
Language
Englisch

Bibliographic citation
“Greener” synthesis of bisphosphonic/dronic acid derivatives ; volume:3 ; number:2 ; year:2014 ; pages:111-116 ; extent:6
Green processing & synthesis ; 3, Heft 2 (2014), 111-116 (gesamt 6)

Creator
Kovács, Rita
Grün, Alajos
Garadnay, Sándor
Greiner, István
Keglevich, György

DOI
10.1515/gps-2013-0107
URN
urn:nbn:de:101:1-2501120303434.388473848885
Rights
Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
Last update
15.08.2025, 7:27 AM CEST

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Associated

  • Kovács, Rita
  • Grün, Alajos
  • Garadnay, Sándor
  • Greiner, István
  • Keglevich, György

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