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  • Title: Synthesis of novel halo and tosyloxy nortropane derivatives as efficient precursors for the one-step synthesis of the dopamine transporter PET ligand [(18)F]FECNT.
    Author: Pijarowska-Kruszyna J, Jaron AW, Kachniarz A, Kasprzak K, Kowalska A, Malkowski B, Demphel S, Dollé F, Mikolajczak R.
    Journal: J Labelled Comp Radiopharm; 2014 Mar; 57(3):148-57. PubMed ID: 24497079.
    Abstract:
    The fluorine-18 labeled nortropane derivative 2β-carbomethoxy-3β-(4-chlorophenyl)-8-(2-fluoroethyl)-nortropane (FECNT) is a dopamine transporter (DAT) ligand. Currently, it is considered as reference for positron emission tomography imaging. Herein, the synthesis of novel precursors (N-tosyloxy-, chloro-, and bromo- analogues) for one-step radiosynthesis of [(18)F]FECNT is reported. Using the N-mesyloxy- precursor in a one-step radiosynthesis, the crude [(18)F]FECNT was obtained with the radiolabeling yield of 45 ± 10%, confirming the practical efficiency of this approach in the design of novel precursors for labeling.
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