title: Carbon-11 radiolabelling of organosulfur compounds: (11) C synthesis of the progesterone receptor agonist tanaproget.
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.
authors.affiliation: Department of Chemistry, Imperial College London, South Kensington, London, SW7 2AZ (UK).
authors.forename: Tom
authors.initials: T
authors.lastname: Haywood
authors.affiliation: Department of Chemistry, Imperial College London, South Kensington, London, SW7 2AZ (UK).
authors.forename: Steven
authors.initials: S
authors.lastname: Kealey
authors.affiliation: Department of Chemistry, Imperial College London, South Kensington, London, SW7 2AZ (UK).
authors.forename: Santiago
authors.initials: S
authors.lastname: Sánchez-Cabezas
authors.affiliation: Department of Chemistry, Imperial College London, South Kensington, London, SW7 2AZ (UK).
authors.forename: James J
authors.initials: JJ
authors.lastname: Hall
authors.affiliation: Institute of Cancer Research, 123 Old Brompton Road, London, SW7 3RP (UK).
authors.forename: Louis
authors.initials: L
authors.lastname: Allott
authors.affiliation: Institute of Cancer Research, 123 Old Brompton Road, London, SW7 3RP (UK).
authors.forename: Graham
authors.initials: G
authors.lastname: Smith
authors.affiliation: Imanova Limited, Burlington Danes Building, Imperial College London, Hammersmith Hospital, Du Cane Road, London, W12 0NN (UK).
authors.forename: Christophe
authors.initials: C
authors.lastname: Plisson
authors.affiliation: Department of Chemistry, Imperial College London, South Kensington, London, SW7 2AZ (UK). philip.miller@imperial.ac.uk.
authors.forename: Philip W
authors.initials: PW
authors.lastname: Miller
mesh_terms: D048588:Benzoxazines / Q000737:chemistry*; D001943:Breast Neoplasms; D002250:Carbon Radioisotopes / Q000737:chemistry*; D006801:Humans; D010296:Parietal Lobe / Q000737:chemistry*; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000737:chemistry*; D011980:Receptors, Progesterone / Q000037:antagonists & inhibitors / Q000737:chemistry*; D013871:Thiones / Q000737:chemistry*; D013890:Thiourea / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D048588:Benzoxazines; D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; D011980:Receptors, Progesterone; D013871:Thiones; D013890:Thiourea; C504446:tanaproget
keywords: carbon; imaging agents; positron emission tomography; radiopharmaceuticals; tanaproget