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Fluorine-18 Radiochemistry, Labeling Strategies and Synthetic Routes
Open accessAbstract
Fluorine-18 is the most frequently used radioisotope in positron emission tomography (PET) radiopharmaceuticals in both clinical and preclinical research. Its physical and nuclear characteristics (97% β(+) decay, 109.7 min half-life, 635 keV positron energy), along with high specific activity and ease of large scale production, make it an attractive nuclide for radiochemical labeling and molecular imaging. Versatile chemistry including nucleophilic and electrophilic substitutions allows direct or indirect introduction of (18)F into molecules of interest. The significant increase in (18)F radiotracers for PET imaging accentuates the need for simple and efficient (18)F-labeling procedures. In this review, we will describe the current radiosynthesis routes and strategies for (18)F labeling of small molecules and biomolecules.
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Tornøe, C. W., Christensen, C., & Meldal, M. (2002) · The Journal of Organic Chemistry · doi:10.1021/jo011148j · Cited by 8,696
Rapid Cu-free click chemistry with readily synthesized biarylazacyclooctynones
Jewett, J. C., Sletten, E. M., & Bertozzi, C. R. (2010) · Journal of the American Chemical Society · doi:10.1021/ja100014q · Cited by 697
Cited by
Wang, Y.-L., Han, Q.-Q., Gong, W.-Q., Pan, D.-H., Wang, L.-Z., Hu, W., Yang, M., Li, B., Yu, J., & Liu, Q. (2018) · Journal of Neuroinflammation · doi:10.1186/s12974-018-1054-3 · Cited by 438
Directed Evolution of a Fluorinase for Improved Fluorination Efficiency with a Non‐native Substrate
Sun, H., Yeo, W. L., Lim, Y. H., Chew, X., Smith, D. J., Xue, B., Chan, K. P., Robinson, R. C., Robins, E. G., Zhao, H., et al. (2016) · Angewandte Chemie International Edition · doi:10.1002/anie.201606722 · Cited by 54
Lowe, P. T., Dall'Angelo, S., Mulder‐Krieger, T., IJzerman, A. P., Zanda, M., & O'Hagan, D. (2017) · ChemBioChem · doi:10.1002/cbic.201700382 · Cited by 19
Metadata
- Authors
- Jacobson, O., Kiesewetter, D. O., & Chen, X.
- Venue
- Bioconjugate Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2014-12-12
- Volume
- 26
- Issue
- 1
- Pages
- 1-18
- ISSN
- 1043-1802 (ISSN-L)
- 1520-4812
- OpenAlex
- W2323389052
- Cited by
- 503
- References
- 2
- FWCI
- 16.36
- Type
- journal article
- Language
- en
- Open access
- hybrid
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