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Synthesis of γ‐amino[4‐ 11 C]butyric acid (GABA)
Author(s) -
Antoni Gunnar,
Långström Bengt
Publication year - 1989
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.2580270510
Subject(s) - chemistry , butyric acid , potassium hydroxide , yield (engineering) , potassium cyanide , tetrahydrofuran , hydrogen cyanide , hydrolysis , cyanoacetic acid , amino acid , cyanide , hydrogen , medicinal chemistry , nuclear chemistry , hydroxide , organic chemistry , solvent , biochemistry , materials science , metallurgy
A one‐pot synthesis of no‐carrier added γ‐amino[4‐ 11 C]butyric acid (GABA) starting with hydrogen [ 11 C]cyanide prepared from [ 11 C]carbon dioxide, is presented. Hydrogen [ 11 C]cyanide was trapped in tetrahydrofuran/potassium hydroxide in the presence of the amino polyether Kryptofix 2.2.2. A Michael addition with ethyl acrylate followed by a selective reduction and hydrolysis of the resulting amino ester gave [4‐ 11 C]GABA. The radiochemical purity of GABA was higher than 99% and the decay corrected radiochemical yield was 60–65% based on the amount of H[ 11 C]CN used. The total synthesis time including purification was around 40 min, counted from the start of the Michael addition reaction.