Opportunities for isotopic labelling via phase‐tagged synthesis with organogermanium linkers | Zendy

Spivey Alan C. | Zendy; Martin Laetitia J. | Zendy; Noban Catherine | Zendy; Jones Teyr C. | Zendy; Ellames George J. | Zendy; Kohler Andrew D. | Zendy

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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.

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