Journal
PHARMACEUTICS
Volume 14, Issue 10, Pages -Publisher
MDPI
DOI: 10.3390/pharmaceutics14102207
Keywords
fluorine-18; amino acids; positron emission tomography; radiopharmaceuticals; radiofluorination
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Funding
- National Natural Science Foundation of China [82171982]
- Natural Science Foundation of Fujian Province [2022J01694]
- Joint Funds for the Innovation of Science and Technology Fujian Province [2020Y9101]
- Fujian Provincial Health Technology Project [2021QNA031]
- Startup Fund for Scientific Research of Fujian Medical University [2020QH1044]
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This review focuses on recent advances in the synthesis, radiolabeling, and application of a series of F-18-labeled amino acid analogs using new F-18-labeling strategies.
Radiolabeled amino acids are an important class of agents for positron emission tomography imaging that target amino acid transporters in many tumor types. Traditional F-18-labeled amino acid synthesis strategies are always based on nucleophilic aromatic substitution reactions with multistep radiosynthesis and low radiochemical yields. In recent years, new F-18-labeling methodologies such as metal-catalyzed radiofluorination and heteroatom (B, P, S, Si, etc.)-F-18 bond formation are being effectively used to synthesize radiopharmaceuticals. This review focuses on recent advances in the synthesis, radiolabeling, and application of a series of F-18-labeled amino acid analogs using new F-18-labeling strategies.
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