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Original Articles

DIRECT RESOLUTION OF ISAMOLTANE (CGP 361A) AND ENCIPRAZINE (WY 48624) ENANTIOMERS, USING CHIRAL HIGH PERFORMANCE LIQUID CHROMATOGRAPHY

, , &
Pages 1877-1892 | Received 27 Jun 1998, Accepted 06 Nov 1998, Published online: 19 Aug 2006
 

Abstract

A chiral high performance liquid chromatography method was developed for the resolution of the enantiomers of two new β-aminoalcohols, isamoltane and enciprazine. The separation of the enantiomers was accomplished, without any derivatization, on a chiral column containing 3,5-dimethylphenylcarbamate of cellulose (Chiralcel OD) as chiral selector.

The effects of diethylamine, organic modifiers (ethanol and 2-propanol) and temperature were studied.

The α 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 used for a semipreparative chromatographic separation to determine the elution order of the enantiomers.

ACKNOWLEDGMENTS

We are grateful to Mrs. A. Mosca for her helpful collaboration and to Novartis Farma and Wyeth-Lederle for having provided us with all the reference standards.

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