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KMID : 1145520160020020137
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Journal of Radiopharmaceuticals and Molecular Probes
2016 Volume.2 No. 2 p.137 ~ p.142
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Fully automated ethanolic loop synthesis of the [11C]OMAR
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Jang Keun-Sam
Song Ho-Chun
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Abstract
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We have successfully synthesized of 4-cyano-1-(2,4-dichlorophenyl)-5-(4-[11C]methoxyphenyl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxzmide ([11C]OMAR), which has been shown a progressing candidate to human brain PET study, from fully automated loop method using ethanol as the only solvent for the entire manufacturing process. The radiochemical yield of [11C]OMAR was observed in 4.1 ± 0.2 % with 4990 ± 384 Ci/mmol of the specific activity and total synthesis time was about 45 minutes after HPLC purification (n = 3, decay corrected) from ethanolic loop system, which was exhibited to better results compared with conventional methods. Ethanolic loop chemistry is favorable and efficient method by simplifies manufacturing procedures as well as satisfied suitable for human administration.
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KEYWORD
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[11C]OMAR, Loop chemistry, Cannabinoid receptor, Positron emission tomography, Green radiochemistry
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