PREPARATION OF 2-[ALPHA-(2-ETHOXYPHENOXY)BENZYL]-[5-C-14]MORPHOLINE METHANESULFONATE ([C-14]REBOXETINE) - A NEW ANTIDEPRESSANT AGENT

The labelling with radiocarbon of the new antidepressant agent Reboxetine is described. The preparation has been carried out in a two step procedure using 2-chloro-N-(3-(2-ethoxyphenoxy)-2-hydroxy-3-phenyl)propyl-[1-C-14]acetamide 2 as starting material. The expected compound was prepared by cyclization of the above halogenoacylamido alcohol to the corresponding morpholone ring followed by reduction to the final [5-C-14]morpholine derivative 4, 98% radiochemically pure and with specific radioactivity of 988 MBq/mmol. An overall radiochemical yield of 57.5% was achieved.