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> or =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.
Sanna
Maria Luisa
ML
Istituto Superiore di Sanità, Dipartimento del Farmaco, Viale Regina Elena 299, 00161 Rome, Italy.
Maccioni
Elias
E
Vigo
Sara
S
Faggi
Cristina
C
Cirilli
Roberto
R
D000688:Amylose / Q000737:chemistry*; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D004353:Drug Evaluation, Preclinical; D008995:Monoamine Oxidase / Q000378:metabolism*; D008996:Monoamine Oxidase Inhibitors / Q000737:chemistry / Q000302:isolation & purification*; D010069:Oxadiazoles / Q000737:chemistry / Q000302:isolation & purification; D013237:Stereoisomerism
D008996:Monoamine Oxidase Inhibitors; D010069:Oxadiazoles; D000688:Amylose; D008995:Monoamine Oxidase