Rodrigo Teodoro, Barbara Wenzel, Arata Oh-Nishi, Steffen Fischer, Dan Peters, Tetsuya Suhara, Winnie Deuther-Conrad, Peter Brust, A high-yield automated radiosynthesis of the alpha-7 nicotinic receptor radioligand [18F]NS10743, Applied Radiation and Isotopes, Volume 95, January 2015, Pages 76-84, ISSN 0969-8043,
F]NS10743, a promising and highly competitive α7 nAChR radioligand has been synthesized so far by microwave irradiation using a manual single-mode device followed by a palladium-catalyzed reduction of remaining nitro-precursor for HPLC separation purposes. For further preclinical and clinical use, regulated production of [18
F]NS10743 by fully automated radiosynthesis is a crucial requirement. Therefore, we chose a commercial synthesis module and developed the automated radiosynthesis of [18
F]NS10743. Besides evaluation of several radiosynthesis procedures, we performed an extensive HPLC study for quantitative separation of [18
F]NS10743 from the corresponding nitro precursor. After implementation of the optimized procedure on a TRACERlabTM FX F-N synthesis module, [18
F]NS10743 was obtained in high radiochemical purity (≥99%) with an overall radiochemical yield of 32.2±7% (n=3). The specific activities at the end of the synthesis were 571±17 GBq/µmol (n=3).
Keywords: Alpha-7 nicotinic acetylcholine receptor radioligand; Pet WAVE microwave CEM®; Radiofluorination; Automated radiosynthesis; TRACERlabTM FX F-N