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Tritium Labelling of Naltrindole, a δ‐Receptor‐Selective Opioid Antagonist via 1‐Bromonaltrexone
Author(s) -
Tóth Géza,
Ötvös Ferenc,
Hosztafi Sándor
Publication year - 1993
Publication title -
helvetica chimica acta
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.74
H-Index - 82
eISSN - 1522-2675
pISSN - 0018-019X
DOI - 10.1002/hlca.19930760612
Subject(s) - naltrindole , chemistry , labelling , moiety , indole test , hydrazine (antidepressant) , tritium , antagonist , stereochemistry , opioid receptor , medicinal chemistry , receptor , biochemistry , physics , nuclear physics
Abstract The synthesis of [1,5′‐ 3 H 2 ]naltrindole ( 9 ) with labels at both the morphine skeleton and the indole moiety was carried out by catalytic tritiodehalogenation of 1,5′‐dibromonaltrindole ( 8 ) resulting in a specific activity of 46.1 Ci/mmol (1705 GBq/mmol). The brominated precursor was prepared by the Fischer indole synthesis starting from 1‐bromonaltrexone ( 7 ) and (4‐bromophenyl)hydrazine.