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Synthesis of N 1 ‐3‐[ 18 F]fluoropropyl‐N 4 ‐2‐([3,4‐dichlorophenyl]ethyl)piperazine, a high affinity ligand for sigma receptor
Author(s) -
Kiesewetter Dale O.,
de Costa Brian
Publication year - 1993
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.2580330711
Subject(s) - chemistry , piperazine , ligand (biochemistry) , yield (engineering) , sigma receptor , high performance liquid chromatography , salt (chemistry) , receptor , stereochemistry , medicinal chemistry , organic chemistry , biochemistry , materials science , metallurgy
The radiochemical synthesis of the high affinity, selective sigma receptor ligand, N 1 ‐3‐[ 18 F]Fluoropropyl‐N 4 ‐2‐([3,4‐dichlorophenyl]ethyl)piperazine, is reported. The labeled compound is prepared by fluoride displacement on a bismethanesulfonate salt of the propyl methanesulfonyloxy precursor. The product is isolated by first passage through a BONDELUT‐SI and subsequently HPLC in high radiochemical and chemical purity with a decay corrected radiochemical yield of 49 ± 9%.