Synthesis of tritium labelled oximes: 2-pyridine aldoxime methiodide (2-PAM) and 1-(2-hydroxyiminomethylpyridinium)-1-(4-carboxyamidopyridinium)dimethylether dichloride (HI-6), with high specific activity
✍ Scribed by Ayala Balan; Itzhak Barness; Gabriel Amitai
- Publisher
- John Wiley and Sons
- Year
- 1993
- Tongue
- French
- Weight
- 441 KB
- Volume
- 33
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
Synthesis of two quaternary pyridinium oximes [^3^H]2‐PAM and [^3^H]HI‐6 (18 and 22 Ci/mmole, respectively) was performed by using unlabelled 6‐bromo 2‐pyridine aldehyde (I) as a common starting material. The labelling was based on a catalytic ring‐tritiation of 6‐bromo 2‐diethylketal pyridine followed by acid hydrolysis and reaction with hydroxylamine to yield 6‐[^3^H]2‐hydroxyiminomethyl pyridine (II). [^3^H]2‐PAM was obtained by reacting II with methyliodide and [^3^H]HI‐6 was prepared by alkylation of II with bischlorodimethylether followed by coupling to isonicotineamide. The radiochemical purity of [^3^H]2‐PAM and [^3^H]HI‐6 was 98% and at least 95% respectively.