Optimized synthesis of N-heterocyclic dronic acids; Closing a black-box era

György Keglevich, Alajos Grün, Klára Aradi, Sándor Garadnay, István Greiner

Research output: Contribution to journalArticle

28 Citations (Scopus)

Abstract

To clarify the inconsistent patent literature, the synthesis of Zoledronic and Risedronic acids involving a heterocyclic acetic acid (HAA), phosphorous acid (PA) and phosphorus trichloride (PC) as the reagents, and methanesulfonic acid as the solvent was studied in detail. It was found that the best synthesis can be accomplished at 80 °C using HAA and PC in a 1:3.1 molar ratio without any PA.

Original languageEnglish
Pages (from-to)2744-2746
Number of pages3
JournalTetrahedron Letters
Volume52
Issue number21
DOIs
Publication statusPublished - May 25 2011

Keywords

  • Dronic acids
  • Mechanism
  • Optimization
  • Rational synthesis

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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