Syntheses of phosphonic esters of alendronate, pamidronate and neridronate

…, N Bouchemal, T Prangé, M Lecouvey

Index: Guenin, Erwann; Monteil, Maelle; Bouchemal, Nadia; Prange, Thierry; Lecouvey, Marc European Journal of Organic Chemistry, 2007 , # 20 p. 3380 - 3391

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Citation Number: 29

Abstract

Abstract Several synthetic pathways for obtaining phosphonic esters of the amino bisphosphonic acids (NBPs) pamidronate, alendronate and neridronate were investigated. The general guideline was to react N-protected amino acids activated as phthalimide esters or as acyl chlorides. Succinimide esters were found less reactive and quickly abandoned. γ- Lactam formation arises when starting from Boc-or Cbz-protected amino acids. The ...