Development novel fluorine-18 labeled artificial amino acid radiopharmaceutical as a tumor seeking PET molecular imaging based on system A amino acid transport

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We have developed [N-methyl-11C]alpha-methylaminoisobutyric acid ([11C]MeAIB) PET imaging as a tumor seeking molecular imaging based on system A amino acid transport. The aim of this study was to develop a new artificial amino acid radiopharmaceutical labeled with fluorine-18, which has longer half-life (109 min) than carbon-11 (20 min) and would be widely available in clinical use. To develop novel fluorine-18 labeled tracers, we focused on alpha-Methyl-DL-serine as a starting material. And then we developed a precursor, (R)-3,4-Dimethyl-1,2,3-oxathiazolidine-4-carboxylic acid tert-butyl ester 2,2-dioxide. Labeling of (R)-3-[18F]Fluoro-2-methyl-2-N-(methylamino)propanoic acid ([18F]NMeFAMP) which are fluorinated analogues of MeAIB was carried out conveniently and efficiently in a short period of time (within 90 min). After the purification, [18F]NMeFAMP was obtained with a radiochemical purity greater than 99.9%.