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Synthesis and 3 H NMR of 3 H‐alaproclate of high specific activity
Author(s) -
Bengtsson Stefan,
Gawell Lars,
Högberg Thomas,
Sahlberg Christer
Publication year - 1985
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.2580220503
Subject(s) - chemistry , tritium , hydrogenolysis , proton nmr , stereochemistry , organic chemistry , catalysis , physics , nuclear physics
Abstract The antidepressant alaproclate (1) is a selective inhibitor of neuronal serotonin reuptake with low affinity for other receptor sites. 3 H‐Alaproclate (3, 2‐([2,5‐ 3 H 2 ]‐4‐chlorophenyl)‐2‐methyl‐2‐propyl 2‐aminopropanoate) with high specific activity (38 Ci/mmol) was prepared by hydrogenolysis of its 2,5‐dibromo analogue 2 with tritium gas. The compound 2 was prepared in a seven step synthesis from 4‐chlorotoluene. The position of the tritium incorporation was verified by 3 H NMR.