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Preparation of 2‐[α‐(2‐ethoxyphenoxy)benzyl]‐[5‐ 14 C]morpholine methanesulfonate ([ 14 C]reboxetine) a new antidepressant agent
Author(s) -
Angiuli Patrizia,
Fontana Erminia,
Vicario Gian Piero
Publication year - 1991
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580290513
Subject(s) - chemistry , reboxetine , yield (engineering) , propiophenone , acetamide , morpholine , carbon 14 , derivative (finance) , radiochemistry , benzyl alcohol , medicinal chemistry , nuclear chemistry , organic chemistry , ketone , catalysis , biochemistry , materials science , receptor , reuptake inhibitor , economics , serotonin , financial economics , metallurgy , physics , quantum mechanics
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.