DIRECT CHROMATOGRAPHIC-SEPARATION OF THE ENANTIOMERS OF PHACLOFEN, SACLOFEN AND HYDROXYSACLOFEN - INFLUENCE OF THE ANIONIC MOIETY

The direct resolution of three analogues of baclofen (phaclofen, saclo fen and hydroxysaclofen), potent gamma-aminobutyric acid B antagonists , is achieved by HPLC on an enantioselective crown ether column. The e ffects of the anionic group are discussed. Perchloric acid and methano l as organic modifier is used as mobile phase. The absolute configurat ion is proposed by comparison with enantiomers of baclofen (beta-p-chl orophenyl-gamma-aminobutyric acid). The above-mentioned compounds are easily and completely resolved.