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Chemistry. 2015 Jun 15;21(25):9034-8. doi: 10.1002/chem.201501089. Epub 2015 May 12.

Carbon-11 radiolabelling of organosulfur compounds: (11) C synthesis of the progesterone receptor agonist tanaproget.

Author information

1
Department of Chemistry, Imperial College London, South Kensington, London, SW7 2AZ (UK).
2
Institute of Cancer Research, 123 Old Brompton Road, London, SW7 3RP (UK).
3
Imanova Limited, Burlington Danes Building, Imperial College London, Hammersmith Hospital, Du Cane Road, London, W12 0NN (UK).
4
Department of Chemistry, Imperial College London, South Kensington, London, SW7 2AZ (UK). philip.miller@imperial.ac.uk.

Abstract

Herein a new (11) C radiolabelling strategy for the fast and efficient synthesis of thioureas and related derivatives using the novel synthon, (11) CS2 , is reported. This approach has enabled the facile labelling of a potent progesterone receptor (PR) agonist, [(11) C]Tanaproget, by the intramolecular reaction of the acyclic aminohydroxyl precursor with (11) CS2 , which has potential applications as a positron emission tomography radioligand for cancer imaging.

KEYWORDS:

carbon; imaging agents; positron emission tomography; radiopharmaceuticals; tanaproget

PMID:
25965348
DOI:
10.1002/chem.201501089
[Indexed for MEDLINE]

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