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KMID : 1145520170030010015
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Journal of Radiopharmaceuticals and Molecular Probes
2017 Volume.3 No. 1 p.15 ~ p.17
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Methodological approaches for the clinical routine production of [11C]raclopride
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Cheong Il-Koo
Lee Ji-Hye
Lee Sang-Yoon
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Abstract
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In carbon-11 labeling, [11C]methyltriflate (methyltrifluoromethanesulfonate, MeOTf) is the most widely used through mild reaction condition with high yield. Strong inorganic bases, KOH, NaH and so on, were chosen to activate precursors that have phenolic alcohol as a nucleophilic moiety, because of its poor nucleophilicity. However, these catalyst can also react with radioactive intermediate, [11C]MeOTf to afford side products. We will briefly discuss the history of the effort to increase the yield of [11C]raclopride and suggest the alternate method for better radiochemical yield and consistency.
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KEYWORD
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[11C]raclopride , Radiochemical yield , Proton sponge , Organic base
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