C - Chemistry – Metallurgy – 07 – F
Patent
C - Chemistry, Metallurgy
07
F
260/501.5
C07F 9/38 (2006.01) C07D 207/404 (2006.01) C07K 5/06 (2006.01) A61K 38/00 (2006.01)
Patent
CA 1106395
ABSTRACT OF THE DISCLOSURE The specification discloses a process for the manufacture of peptide derivatives of the general formula Image (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.
282222
Atherton Frank R.
Hall Michael J.
Hassall Cedric H.
Lambert Robert W.
Ringrose Peter S.
Gowling Lafleur Henderson Llp
Hoffmann-La Roche Limited
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