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Carbon‐11 Radiolabelling of Organosulfur Compounds: 11 C Synthesis of the Progesterone Receptor Agonist Tanaproget
Author(s) -
Haywood Tom,
Kealey Steven,
SánchezCabezas Santiago,
Hall James J.,
Allott Louis,
Smith Graham,
Plisson Christophe,
Miller Philip W.
Publication year - 2015
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201501089
Subject(s) - synthon , chemistry , agonist , radioligand , organosulfur compounds , pet imaging , stereochemistry , combinatorial chemistry , positron emission tomography , receptor , organic chemistry , sulfur , biochemistry , nuclear medicine , medicine
Herein a new 11 C radiolabelling strategy for the fast and efficient synthesis of thioureas and related derivatives using the novel synthon, 11 CS 2 , 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 CS 2 , which has potential applications as a positron emission tomography radioligand for cancer imaging.