Direct resolution of isamoltane (CGP 361A) and enciprazine (WY 48624) enantiomers, using chiral high performance liquid chromatography

A chiral high performance liquid chromatography method was developed for th e resolution of the enantiomers of two new beta-aminoalcohols, isamoltane a nd enciprazine. The separation of the enantiomers was accomplished, without any derivatization, on a chiral column containing 3,5-dimethylphenylcarbam ate of cellulose (Chiralcel OD) as chiral selector. The effects of diethylamine, organic modifiers (ethanol and 2-propanol) and temperature were studied. The alpha and Rs values of isamoltane and enciprazine ranged, respectively, from 1.25 to 2.03 and from 0.80 to 5.16. The optimized conditions were use d for a semipreparative chromatographic separation to determine the elution order of the enantiomers.