ACIDES AMINES FLUORES

摘要

1367674 3-Fluoro-alanines MERCK & CO Inc 26 July 1971 [3 Aug 1970 3 June 1971] 34886/71 Heading C2C Novel D-isomers of the formula wherein each of x and y is 1 or 2 (thus each of x and y represent hydrogen or deuterium) and pharmaceutically acceptable salt thereof are prepared: (a) by the action of fluoroxyperfluoroalkane or fluoroxypentafluorosulphur on D- alanine under free radical initiation followed by chromatographic separation of the product to isolate 3-fluoro-alanine; (b) by the action of alanine racemase (an enzyme preparation from Staphylococcus aureus) in 2H 2 O on L-alanine to incorporate deuterium into the alpha-position of D-alanine (the deuterated D-alanine is separated by the sequence N-acetylation, chromatographic separation and deacetylation), the thus produced 2-2H-D-alanine in subjected to the procedure under (a) above to form 2-2H-3-fluoro-D- alanine; and (c) 3,3,3-2H-D-alanine (obtained by the resolution of perdeutero alanine racemate using the sequence N-acetylation and deacetylation) is fluorinated as in (a) to form 3,3,2-2H- 3-fluoro-D-alanine. Pharmaceutical compositions and disinfectant compositions having anti-bacterial activity comprise the above novel compounds and a carrier therefore.