PERFLUOROALKYL SUBSTITUTED METALLO-BETA-LACTAMASE INHIBITORS AND METHOD FOR THE PREPARATION OF TRIFLUOROMETHYLKETONE DERIVATIVES

摘要

The invention concerns perfluoro-lower-alkyl derivatives of amino acids. A new synthetic route is provided for preparing alpha -aminotrifluoromethylketones, by converting alpha -amino acids to oxazolidin-5-ones which are then reacted with Ruppert's Reagent. Fluorinated derivatives of amino acids and peptides are shown to have a new property of inhibiting or inactivating metallo- beta -lactamase enzymes, and are thus valuable components of antibacterial formulations. Certain of the trifluoromethyl derivatives of amino acids are new compounds per se.