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Abstract

[11C]Raclopride is one of the most popular PET tracers used in Parkinson's disease studies. We previously prepared [11C]raclopride with reasonable yields using NaOH as an inorganic base, but the reaction patterns fluctuated. In this study, we describe the successful application of a commercially available 'super basic' proton sponge, TMGN, as a base for the [11C]methylation step using [11C]CH3OTf. This novel TMGN method produced better radiochemical yields, as well as enhanced reproducibility and a reduction in side products. Under optimal conditions (1.2 equiv. of TMGN), the radiochemical yield was 14.4±0.2% (ndc, EOS, n=5) and the specific activity was 66.6±13.3 GBq/mmol (n=5).​ 

Author information

Lee J1, Cheong IK2, Lee SY3.​

1Neuroscience Research Institute, Gachon University, 24, Namdong-daero 774 beon-gil, Namdong-gu, Incheon, Korea.

2Gachon Advanced Institute for Health Science and Technology, Graduate School, Gachon University, 155, Gaetbeol-ro, Yeonsu-gu, Incheon, Korea.

3Neuroscience Research Institute, Gachon University, 24, Namdong-daero 774 beon-gil, Namdong-gu, Incheon, Korea; Department of Neuroscience, College of Medicine, Gachon University, 191, Hambangmoe-ro, Yeonsu-gu, Incheon, Korea. Electronic address: rchemist@gachon.ac.kr.