Derivatization of (±)-5-[(2-methylphenoxy)methyl]-2-amino-2-oxazoline, an imidazoline binding sites ligand, with (+)-(R)-α-methylbenzyl isocyanate for drug monitoring purposes

Abstract

The derivatization of racemic 5-[(2-methylphenoxy)-methyl]-2-amino-2-oxazoline, developed as an imidazoline binding sites ligand, with (+)-(R)-α-methylbenzyl isocyanate was performed in chloroform. The reaction led to two pairs of diastereomers, which were separated by RP-HPLC. A kinetic study of the derivatization reaction was achieved in order to establish conditions suitable for experimental drug monitoring.