Synthesis of novel halo and tosyloxy nortropane derivatives as efficient precursors for the one‐step synthesis of the dopamine transporter PET ligand [18F]FECNT
作者： J. Pijarowska-Kruszyna , A. W. Jaron , A. Kachniarz , K. Kasprzak , A. Kowalska
DOI: 10.1002/JLCR.3181
关键词:
摘要: The fluorine-18 labeled nortropane derivative 2β-carbomethoxy-3β-(4-chlorophenyl)-8-(2-fluoroethyl)-nortropane (FECNT) is a dopamine transporter (DAT) ligand. Currently, it considered as reference for positron emission tomography imaging. Herein, the synthesis of novel precursors (N-tosyloxy-, chloro-, and bromo- analogues) one-step radiosynthesis [(18)F]FECNT reported. Using N-mesyloxy- precursor in radiosynthesis, crude was obtained with radiolabeling yield 45 ± 10%, confirming practical efficiency this approach design labeling.
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