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Opportunities for isotopic labelling via phase‐tagged synthesis with organogermanium linkers
Author(s) -
Spivey Alan C.,
Martin Laetitia J.,
Noban Catherine,
Jones Teyr C.,
Ellames George J.,
Kohler Andrew D.
Publication year - 2007
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.1302
Subject(s) - chemistry , rimonabant , antagonist , labelling , adme , combinatorial chemistry , stereochemistry , chemical synthesis , receptor , biochemistry , cannabinoid receptor , in vitro
Strategies for the use of germanium‐based linkers for the phase‐tagged synthesis of isotopically labelled intermediates are described. Protocols of potential use in the devolatilization of volatile intermediates prepared from [ 14 C]‐CO 2 and [ 14 C]‐PhBr to aid ADME studies on drug substances and their metabolites are discussed in relation to SR47035 (an advanced intermediate en‐route to the 5‐HT 2 receptor antagonist SR46349B) and 4‐amino‐4‐phenylpiperidine (a key intermediate in the synthesis of NK 3 receptor antagonist SR142801, osanetant). Additionally, protocols with potential for the preparation of [ 123 I] and [ 18 F]‐labelled SPECT/PET imaging/diagnostic agents are discussed in relation to an [ 123 I]‐labelled analogue of SR141716 (rimonabant, a CB 1 receptor antagonist) and 6‐[ 18 F]‐( S )‐DOPA (for diagnosis of Parkinson's disease). Copyright © 2007 John Wiley & Sons, Ltd.