Haywood Tom, Kealey Steven, Sánchez-Cabezas Santiago, Hall James J, Allott Louis, Smith Graham, Plisson Christophe, Miller Philip W
Department of Chemistry, Imperial College London, South Kensington, London, SW7 2AZ (UK).
Institute of Cancer Research, 123 Old Brompton Road, London, SW7 3RP (UK).
Chemistry. 2015 Jun 15;21(25):9034-8. doi: 10.1002/chem.201501089. Epub 2015 May 12.
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.
本文报道了一种使用新型合成子(11)C二硫化碳快速高效合成硫脲及相关衍生物的新的(11)C放射性标记策略。该方法通过无环氨基羟基前体与(11)C二硫化碳的分子内反应，实现了一种有效的孕酮受体(PR)激动剂[(11)C]他那孕酮的简便标记，其作为用于癌症成像的正电子发射断层扫描放射性配体具有潜在应用价值。
