Successful application of a neutral organic base, 1,8-bis(tetramethylguanidino)naphthalene (TMGN), for the radiosynthesis of [C-11]raclopride
- Authors
- Lee, Jihye; Cheong, Il-Koo; Lee, Sang-Yoon
- Issue Date
- Dec-2016
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- [C-11]Raclopride; PET imaging; Parkinson' s disease; Proton sponge; TMGN
- Citation
- APPLIED RADIATION AND ISOTOPES, v.118, pp.382 - 388
- Journal Title
- APPLIED RADIATION AND ISOTOPES
- Volume
- 118
- Start Page
- 382
- End Page
- 388
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/7640
- DOI
- 10.1016/j.apradiso.2016.10.006
- ISSN
- 0969-8043
- Abstract
- [C-11]Raclopride is one of the most popular PET tracers used in Parkinson's disease studies. We previously prepared [C-11]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 [C-11]methylation step using [C-11]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).
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