Safety-catch linker strategies for the production of radiopharmaceuticals labeled with positron-emitting isotopes.
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.
Maclean
Derek
D
Affymax Research Institute, 4001 Miranda Avenue, Palo Alto, California 94304, USA. maclean@netcom.com
Zhu
Jiang
J
Chen
Mingying
M
Hale
Ron
R
Satymurthy
Nagichettiar
N
Barrio
Jorge R
JR
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
D003432:Cross-Linking Reagents; D006847:Hydrocarbons, Iodinated; D019275:Radiopharmaceuticals; C014055:methyl iodide