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Radiosynthesis of a new radiobrominated ligand for 5HT 2A receptors, a potential tracer for PET
Author(s) -
Terriere D.,
Hermanne A.,
Sonck M.,
Leysen J. E.,
Mertens J.
Publication year - 1997
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/(sici)1099-1344(199701)39:1<11::aid-jlcr943>3.0.co;2-g
Subject(s) - chemistry , peracetic acid , hydrogen peroxide , benzamide , acetic acid , radiosynthesis , ligand (biochemistry) , yield (engineering) , quipazine , chemical synthesis , labelling , receptor , stereochemistry , medicinal chemistry , combinatorial chemistry , nuclear chemistry , organic chemistry , serotonin , 5 ht receptor , biochemistry , microbiology and biotechnology , in vivo , biology , materials science , metallurgy , in vitro
4‐Amino‐N‐[1‐[3‐(4‐fluorophenoxy)propyl]‐4‐methyl‐4‐piperidinyl]‐2‐methoxy‐benzamide, a compound with high affinity for 5HT 2 ‐receptors, was radiobrominated in the 5‐position of the methoxybenzamide group by electrophilic substitution. Hydrogen peroxide / acetic acid, peracetic acid and a mixture of both were tried as oxidants. Radiobromination with the hydrogen peroxide method gave a labelling yield of 80 % in the 5‐position and 20 % in the 3‐position without any side products. On the other hand the labelling methods based on the use of peracetic acid gave a more selective radiobromination in the 5‐position, but with low yields and moreover generated radioactive and non‐radioactive side products. N.C.A. radiobromide of high radio‐chemical purity was obtained by an ion‐exchange procedure on the target material solution coupled to a purification step using methanol. © 1997 John Wiley & Sons, Ltd.