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- Title
Simple preparation of new [<sup>18</sup>F]F-labeled synthetic amino acid derivatives with two click reactions in one-pot and SPE purification.
- Authors
Yook, Cheol ‐ Min; Lee, Sang Ju; Oh, Seung Jun; Ha, Hyun ‐ Joon; Lee, Jong Jin
- Abstract
New [18F]fluorinated 1,2,3-triazolyl amino acid derivatives were efficiently prepared from Huisgen 1,3-dipolar cycloaddition reactions, well known as click reaction. We developed two simultaneous click reactions in one-pot with a simple solid-phase extraction (SPE) purification method. [18F]fluoro-1-propyne was obtained at a 45% non-decay corrected radiochemical yield based on the [18F]fluoride ion. The one-pot and simultaneous two click reactions were performed with unprotected azido-alkyl amino acid, [18F]fluoro-1-propyne, and lipophilic additive alkyne to produce three synthetic amino acid derivatives, AMC-101 ( [18F]-6a), AMC-102 ( [18F]-6b), and AMC-103 ( [18F]-6c) with 29%, 28%, and 24% of non-decay corrected radiochemical yields, respectively. All radiotracers indicated that radiochemical purities were >95% without any residual organic solvent. Our new method involving two click reactions in one-pot showed high radiochemical and chemical purity by easy removal of the residual precursor from the simultaneous two click reactions.
- Subjects
AMINO acid synthesis; AMINO acid analysis; AMINO acid derivatives; PHYSIOLOGICAL effects of amino acids; SOLID phase extraction
- Publication
Journal of Labelled Compounds & Radiopharmaceuticals, 2015, Vol 58, Issue 8, p317
- ISSN
0362-4803
- Publication type
Article
- DOI
10.1002/jlcr.3297