title: Safety-catch linker strategies for the production of radiopharmaceuticals labeled with positron-emitting isotopes.
abstract: 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.
authors.affiliation: Affymax Research Institute, 4001 Miranda Avenue, Palo Alto, California 94304, USA. maclean@netcom.com
authors.forename: Derek
authors.initials: D
authors.lastname: Maclean
authors.forename: Jiang
authors.initials: J
authors.lastname: Zhu
authors.forename: Mingying
authors.initials: M
authors.lastname: Chen
authors.forename: Ron
authors.initials: R
authors.lastname: Hale
authors.forename: Nagichettiar
authors.initials: N
authors.lastname: Satymurthy
authors.forename: Jorge R
authors.initials: JR
authors.lastname: Barrio
mesh_terms: D000478:Alkylation; D003432:Cross-Linking Reagents / Q000737:chemistry*; D006847:Hydrocarbons, Iodinated / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D014055:Tomography, Emission-Computed / Q000379:methods
chemical_list: D003432:Cross-Linking Reagents; D006847:Hydrocarbons, Iodinated; D019275:Radiopharmaceuticals; C014055:methyl iodide