Synthesis of novel halo and tosyloxy nortropane derivatives as efficient precursors for the one??step synthesis of the dopamine transporter PET ligand [18F] FECNT

J Pijarowska??Kruszyna, AW Jaron…

Index: Pijarowska-Kruszyna; Jaron; Kachniarz; Kasprzak; Kowalska; Malkowski; Demphel; Dolle; Mikolajczak Journal of Labelled Compounds and Radiopharmaceuticals, 2014 , vol. 57, # 3 p. 148 - 157

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Citation Number: 3

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 [18F] FECNT is reported. Using the N-mesyloxy-precursor in a one-step radiosynthesis, ...