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Radiosynthesis of a ligand for studying the glycine transporter: [ 11 C]ALX‐5407
Author(s) -
Ravert Hayden T.,
Mathews William B.,
Klitenick Mark A.,
Wong Dean F.,
Dannals Robert F.
Publication year - 2001
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.453
Subject(s) - chemistry , sarcosine , saponification , radiosynthesis , glycine , desmethyl , yield (engineering) , ligand (biochemistry) , alkylation , transporter , specific activity , radiochemistry , medicinal chemistry , stereochemistry , organic chemistry , receptor , amino acid , biochemistry , in vivo , materials science , microbiology and biotechnology , metabolite , gene , metallurgy , biology , enzyme , catalysis
[ 11 C]ALX‐5407, R‐ N [3‐(4′‐fluorophenyl)‐3‐(4′‐phenylphenoxy)propyl] sarcosine, a chiral glycine transporter 1 antagonist, was labeled with [ 11 C]iodomethane by N‐alkylation of methyl ester protected N‐normethyl precursor, ALX‐5536, and subsequent saponification of the methyl ester protecting group. The time for synthesis, purification, and formulation was 33 minutes with an average specific radioactivity of 3909 mCi/µmol (EOS) and average decay corrected radiochemical yield of 8%. Copyright © 2001 John Wiley & Sons, Ltd.