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Abstract
The preparative enantiomeric resolution of two analogues of baclofen: saclofen and hydroxysaclofen, potent γ-aminobutyric acid B (GABA B) antagonists, was obtained by HPLC with an analytical crown ether column (CR+) using isocratic conditions and multiple repetitive injections. The preparative separation was optimized by adjusting the sample size, by detecting the sample where its UV absorbance was low and from a scale-up of the analytical method. The analytical separation was modified to provide a convenient method for the isolation of the two enantiomers. The best analytical results obtained were α = 3.68, R s = 20.96 with H 2OCH 3OH (90:10) at 0.5 ml/min and 20°C for hydroxysaclofen. Suitable fractionation allowed the isolation of pure (>99%) enantiomers for pharmacological testing.
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