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Synthesis of 77Br-labelled 2-(4-bromo-2,5-dimethoxyphenyl)-isopropylamine with high specific activity

✍ Scribed by H. H. Coenen

Publisher
John Wiley and Sons
Year
1981
Tongue
French
Weight
273 KB
Volume
18
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The tagging of 2,5‐dimethoxyphenylisopropylamine (DPIA) with bromine‐77 (T~1/2~ = 56 hrs) was reinvestigated in order to achieve high specific activities which are necessary for in‐vivo application of this centrally acting drug. A fast one‐pot synthesis was developed using N‐chlorotetrafluorosuccinimide (NCTFS) and practically carrier‐free bromide to introduce radiobromide into the aromatic ring. Trifluoroacetic anhydride (TFA) was applied both as solvent and as a reversible blocking agent of the free amino group. TFA was also shown to suppress chlorinating sidereactions. Rapid separation of 4‐^77^Br‐2,5‐dimethoxyphenylisopropylamine was achieved by reverse phase high pressure liquid chromatography. The total labelling and separation procedure takes about two hours, and 4‐^77^Br‐DOB is obtained with an overall radiochemical yield of 25% and a specific activity of <8 Ci/μmole.

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