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Synthesis of 3H-labeled sympathomimetic amines for neuronal mapping

✍ Scribed by Marcian E. Van Dort; David L. Gildersleeve; Donald M. Wieland

Publisher
John Wiley and Sons
Year
1990
Tongue
French
Weight
443 KB
Volume
28
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The synthesis of two tritium labeled sympathomimetic amines, (R)‐(‐)‐phenylephrine and (1R,2S)‐(‐)‐meta‐hydroxyephedrine, is described. The tritium label was introduced into the aromatic ring in the final step by catalytic reductive dehalogenation of the corresponding iodinated precursor. (1R,2S)‐(‐)‐meta‐hydroxyephedrine was synthesized in four steps from commercially available metaraminol. A novel HPLC purification method provided the labeled compounds in a medium ready for direct animal evaluation. Chemical and radiochemical purity was ≥98%; specific activity was ≥ 22 Ci/mmol.

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