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

Autor: J. W. Faigle, W. Küng, B. Wirz, E. Kocher
Rok vydání: 1983
Předmět:
Zdroj: Journal of Labelled Compounds and Radiopharmaceuticals. 20:213-231
ISSN: 0362-4803
DOI: 10.1002/jlcr.2580200209
Popis: 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 14CO2. The total radiochemical yield is 30%, calculated from the first labelled intermediate, i.e. 4-chlorobenzoic acid. Second, the 14C-atom is incorporated in the 4-position of the acid chain through three steps only, using K14CN 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.
Databáze: OpenAIRE