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Synthesis of carbon-14- and tritium-labelled 4-amino-3- (4-chlorophenyl) -butyric acid (baclofen)

✍ Scribed by W. Küng; J. W. Faigle; E. Kocher; B. Wirz

Publisher
John Wiley and Sons
Year
1983
Tongue
French
Weight
519 KB
Volume
20
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Two preparations of carbon‐14 labelled 4‐amino‐3‐(4‐chlorophenyl)‐butyric acid are described : First, the label is introduced in the 3‐position of the butyric acid chain in nine steps, starting from ^14^CO~2~. The total radiochemical yield is 30%, calculated from the first labelled intermediate, i.e. 4‐chlorobenzoic acid. Second, the ^14^C‐atom is incorporated in the 4‐position of the acid chain through three steps only, using K^14^CN as starting material with a yield of 39%.

Synthesis of the title compound labelled with tritium in the benzene nucleus is performed by catalytic bromine‐tritium exchange, affording a product with a specific radioactivity of 9.38 Ci/mmol. The des‐chloro compound which is obtained as a by‐product, is separated by column chromatography.

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