Application of an immobilised amylose-based chiral stationary phase to the development of new monoamine oxidase B inhibitors

A direct HPLC enantioseparation of three new chiral oxadiazoline derivatives endowed with potential MAO-B inhibitory activity was accomplished on the immobilised Chiralpak IA chiral stationary phase. Multi-mg amounts of enantiomers with high enantiomeric purity (ee ≥ 98%) were rapidly collected usin...

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Veröffentlicht in:	Talanta (Oxford) 2010-06, Vol.82 (1), p.426-431
Hauptverfasser:	Sanna, Maria Luisa, Maccioni, Elias, Vigo, Sara, Faggi, Cristina, Cirilli, Roberto
Format:	Artikel
Sprache:	eng
Schlagworte:	Absolute configuration Amylose - chemistry Analytical chemistry Chemistry Chiralpak IA Chiroptical properties Chromatographic methods and physical methods associated with chromatography Chromatography, High Pressure Liquid - methods Drug Evaluation, Preclinical Enantiomers Enantioselective HPLC Exact sciences and technology MAO-inhibitors Monoamine Oxidase - metabolism Monoamine Oxidase Inhibitors - chemistry Monoamine Oxidase Inhibitors - isolation & purification Other chromatographic methods Oxadiazoles - chemistry Oxadiazoles - isolation & purification Stereoisomerism
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Zusammenfassung:	A direct HPLC enantioseparation of three new chiral oxadiazoline derivatives endowed with potential MAO-B inhibitory activity was accomplished on the immobilised Chiralpak IA chiral stationary phase. Multi-mg amounts of enantiomers with high enantiomeric purity (ee ≥ 98%) were rapidly collected using pure dichloromethane as eluent. The absolute configuration and chiroptical properties of the enantiomers isolated at semipreparative scale were exhaustively determined.
ISSN:	0039-9140 1873-3573
DOI:	10.1016/j.talanta.2010.04.039