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Preparation of 2-[α-(2-ethoxyphenoxy)benzyl]-[5-14C]morpholine methanesulfonate ([14C]reboxetine) a new antidepressant agent

✍ Scribed by Patrizia Angiuli; Erminia Fontana; Gian Piero Vicario

Publisher
John Wiley and Sons
Year
1991
Tongue
French
Weight
213 KB
Volume
29
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

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‐^14^C]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‐^14^C]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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