Premium
Synthesis of carbon‐14‐ and tritium‐labelled 4‐amino‐3‐ (4‐chlorophenyl) ‐butyric acid (baclofen)
Author(s) -
Küng W.,
Faigle J. W.,
Kocher E.,
Wirz B.
Publication year - 1983
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580200209
Subject(s) - chemistry , tritium , butyric acid , yield (engineering) , benzene , radiochemistry , specific activity , carbon fibers , catalysis , organic chemistry , physics , materials science , composite number , nuclear physics , metallurgy , composite material , enzyme
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.