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Synthesis of [77Br] 5,7-dibromo-4-oxo-1,4-dihydroquinoline-2-carboxylic acid, a possible SPECT tracer for NMDA receptor studies

✍ Scribed by F. Dumont; G. Slegers

Publisher: John Wiley and Sons
Year: 1996
Tongue: French
Weight: 272 KB
Volume: 38
Category: Article
ISSN: 0022-2135
DOI: 10.1002/(sici)1099-1344(199609)38:9<795::aid-jlcr891>3.0.co;2-2

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✦ Synopsis

The synthesis of [77Br] 5,7-dibromo-4-oxo-1,4-dihydroquinoline-2-carboxylic acid is described. The labelling is performed in order to obtain a tracer for SPECT studies of the Nmethyl-D-aspartate receptor in human brain. Radiosynthesis was carried out using a nonisotopic nucleophilic halogen exchange, starting from 5-iodo-7-bromo-4-oxo-1,4dihydroquinoline-2-carboxylic acid. In order to obtain the best radiochemical yield, several parameters such as reaction temperature, reaction time, amount of precursor and amount of Cu catalyst were studied. Under the best labelling conditions, the radiochemical yield was 85 %. The product was found to be chemically and radiochemically pure as determined by HPLC.

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