Journal of Enzyme Inhibition and Medicinal Chemistry 2002-12-01

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

Myriam Matoga, Isabelle Forfar, Corinne Chaimbault, Jean Guillon, Fabienne Péhourcq, Jean-Jacques Bosc, Marie-Claire Rettori, Christian Jarry

Index: J. Enzyme Inhib. Med. Chem. 17(6) , 375-9, (2002)

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Abstract

The derivatization of racemic 5-[(2-methylphenoxy)methyl]-2-amino-2-oxazoline, developed as an imidazoline binding sites ligand, with (+)-(R)-alpha-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.