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A convenient method for the specific tritium labelling of beta‐adrenoceptor antagonists
Author(s) -
Arfwidsson Anders,
Hallhagen Göran,
Hoffmann KurtJürgen
Publication year - 1980
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.2580170308
Subject(s) - chemistry , labelling , alprenolol , tritium , sodium borohydride , reagent , tritium illumination , beta (programming language) , radiochemistry , stereochemistry , combinatorial chemistry , organic chemistry , biochemistry , receptor , nuclear physics , physics , computer science , programming language , catalysis
The specific tritium labelling of beta‐adrenoceptor antagonists of the general structure ArOCH 2 CH(OH)CH 2 NHR is described. The tritium label is introduced in the 2‐position in the aminohydroxypropoxy side‐chain starting from ArOCH, an intermediate in the synthesis of the unlabelled compound. The key step is a reduction of the corresponding bromoketone ArOCH 2 COCH 2 Br using readily available sodium borohydride‐ 3 H as the labelling reagent. The 2‐position has proven stable enough to be suitable for most biochemical applications, e.g. metabolic studies. Five examples are given, including alprenolol‐ 3 H and metoprolol‐ 3 H.