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‐[1‐14C]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 [5‐14C]morpholone derivative 4, 98% radiochemically pure and with specific radioactivity of 988 MBq/mmol. An overall radiochemical yield of 57.5% was achieved.
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Angiuli et al. (1991) studied this question.