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Synthesis of [3H]naltrindole [1]

✍ Scribed by Clifford R. Dorn; Charles S. Markos; Michael S. Dappen; Barnett S. Pitzele

Publisher
John Wiley and Sons
Year
1992
Tongue
French
Weight
287 KB
Volume
31
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

[^3^H]Naltrindole ([^3^H]1) was prepared for use as a selective radiolabeled ligand for delta opioid receptors. The Fischer indole synthesis from naltrexone and 2,4‐dibromophenylhydrazine produced dibromide precursor 2, which was catalytically dehalogenated with carrier free tritium gas to afford [^3^H]1 in 45.8% yield at a specific activity of 39.5 Ci/mmol.

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