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A convenient method for the specific tritium labelling of beta-adrenoceptor antagonists

✍ Scribed by Anders Arfwidsson; Göran Hallhagen; Kurt-Jürgen Hoffmann

Publisher
John Wiley and Sons
Year
1980
Tongue
French
Weight
461 KB
Volume
17
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

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.

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