PHOSPHONIC ACID PEPTIDE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

摘要

The specification discloses a process for the manufacture of peptide derivatives of the general formula (I) , especially for the manufacture of (D,L-3-fluoroalanylamino)-methylphosphonic acid and (1R)-1-(L-3-fluoroalanylamino)-ethyl-phosphonic acid and of pharmaceutically acceptable salts thereof. The hydrogenolytically cleavable N-protecting group of N-protected (D,L-3-fluoroalanylamino)-methylphospnonic acid or (1R)-1-(L-3-fluoroalanylamino)-ethylphosphonic acid is cleaved off by hydrogenolysis. If desired the compound obtained is converted into a pharmaceutically acceptable salt. The compounds obtained in accordance with the claimed process are antibacterially active and they are found to potentiate the activity of antibiotics.