Rational synthesis of Ibandronate and Alendronate

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

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Abstract

Ibandronate and Alendronate/Alendronic acid were prepared by the reaction of the corresponding amino acids (N-methyl-N-pentylalanine and γ-aminobutyric acid) with 3.2 equivalents of phosphorus trichloride, in the absence of any phosphorous acid, in methanesulfonic acid at 75 °C for 12 h followed by hydrolysis, pH adjustment and purification. The first intermediate of the reaction sequence is the corresponding chloride (>N(CH2)nC(O)Cl) or mixed ester (>N(CH2)nC(O)OS(O) 2Me).

Original languageEnglish
Pages (from-to)640-644
Number of pages5
JournalCurrent Organic Synthesis
Volume10
Issue number4
DOIs
Publication statusPublished - Jan 1 2013

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Keywords

  • Alendronate
  • Ibandronate
  • Intermediate
  • Optimization
  • Synthesis

ASJC Scopus subject areas

  • Biochemistry
  • Organic Chemistry

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