Enantiomeric resolution of melatonin ligands receptors by liquid chromatography on amylose chiral stationary phases

Analytical HPLC methods using derivatized amylose chiral stationary phases were developed for the resolution of enantiomers of methoxy an ethyl tetrah ydronaphthalenic derivatives, new agonist and antagonist ligands for melato nin receptors. Separation was by normal phase methodology with a mobile pha se of n-hexane-alcohol (methanol, ethanol,1-propanol or 2-propanol) in vari ous proportions, and a silica-based, amylose tris-(S)-1-phenylethylcarbamat e (Chiralpak AS), or tris-3,5-dimethylphenylcarbamate (Chiralpak AD). The m obile phase and the chiral stationary phase were optimized for best resolut ion. The effects of concentration of alcohol, various aliphatic alcohols in the mobile phase were studied. The effects of substitution were analysed. Baseline separation (R-s > 1.5) was easily obtained in many cases.