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Safety-Catch Linker Strategies for the Production of Radiopharmaceuticals Labeled with Positron-Emitting Isotopes

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journal contribution
posted on 31.07.2003, 00:00 by Derek Maclean, Jiang Zhu, Mingying Chen, Ron Hale, Nagichettiar Satymurthy, Jorge R. Barrio
A novel synthetic stratetegy for compounds labeled with the positron-emitting isotope carbon-11 is described. The use of precursors attached to a solid support via safety-catch linkers allows selective release of radiolabeled material, leaving unreacted precursor attached to the support. Two different linkers demonstrate the application to the preparation of radiolabeled N-alkyl tertiary amines and N-alkylsulfonamides. This technique is expected to lead to more widespread use of positron emission tomography for the in vivo analysis of compound behavior.