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Published on: December 15, 2017
Development and optimization of a novel automated loop method for production of [11C]nicotine
Arijit Ghosh1, Karen Woolum1, Michael V Knopp1
1Laboratory for Translational Research in Imaging Pharmaceuticals, The Wright Center of Innovation in Biomedical Imaging, Department of Radiology, The Ohio State University, Columbus, OH 43212, United States.
Abstract:
A novel, rapid, and automated loop method for the synthesis of [11C]nicotine was developed and optimized. The method involves, a reaction of the precursor, (+) nornicotine or (-) nornicotine, with a gas-phase produced [11C]CH3I in an 800 µL loop at 75 °C for 5 min followed by a semi-preparatory Reversed-Phase High-Performance Liquid Chromatography (RP-HPLC) purification. The optimized synthesis and purification process was complete in < 30 min and produced [11C]nicotine with > 99.9% Radiochemical Purity (RCP), no [11C]CH3I, no (+) nornicotine, 105 mCi/µmole specific activity, 7.0 - 7.2 pH, and 16.6% ethanol. The current method can be optimized, to reduce the ethanol content (<10%), and can be translated to a cGMP production of [11C]nicotine for human clinical trials.
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