Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
8208513 | Applied Radiation and Isotopes | 2018 | 19 Pages |
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 800â¯ÂµL loop at 75â¯Â°C for 5â¯min followed by a semi-preparatory Reversed-Phase High-Performance Liquid Chromatography (RP-HPLC) purification. The optimized synthesis and purification process was complete in <â¯30â¯min and produced [11C]nicotine with >â¯99.9% Radiochemical Purity (RCP), no [11C]CH3I, no (+) nornicotine, 105â¯mCi/µmole specific activity, 7.0 - 7.2â¯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.
Keywords
Related Topics
Physical Sciences and Engineering
Physics and Astronomy
Radiation
Authors
Arijit Ghosh, Karen Woolum, Michael V. Knopp, Krishan Kumar,