Syntheses of F-18 labeled fluoroalkyltyrosine derivatives and their biological evaluation in rat bearing 9L tumor |
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| Authors: | Moon Byung Seok Lee Tae Sup Lee Kyo Chul An Gwang Il Cheon Gi Jeong Lim Sang Moo Choi Chang Woon Chi Dae Yoon Chun Kwon Soo |
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| Institution: | Laboratory of Radiopharmaceuticals, Korea Institute of Radiological and Medical Sciences, 215-4 Gongneungdong, Nowongu, Seoul 139-706, Republic of Korea. |
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| Abstract: | We hereby report the synthesis of four fluorine-18 labeled tyrosine derivatives, 3-(2-(18)F]fluoroethyl)tyrosine ((18)F]1, (18)F]ortho-FET), 3-(3-(18)F]fluoropropyl)tyrosine ((18)F]2, (18)F]ortho-FPT) O-methyl-3-(2-(18)F]fluoroethyl)]tyrosine ((18)F]3, (18)F]MFET), and O-methyl-3-(3-(18)F]fluoropropyl)]tyrosine ((18)F]4, (18)F]MFPT). The fluorine-18 labeled tyrosine derivatives were prepared by the displacement reaction of the ethyl and propyl tosylates with K(18)F]/K2.2.2 in acetonitrile under no-carrier-added (NCA) conditions, followed by hydrolysis with 4N HCl. The biological properties of labeled compounds were evaluated in rats bearing 9L tumor after an intravenous injection and PET image was obtained. The tumor/blood and tumor/brain ratios were 2.06, 2.92 for (18)F]1, 2.25, 4.05 for (18)F]2, 2.88, 1.90 for (18)F]3, and 2.00, 2.60 for (18)F]4 at 60 min post injection, respectively. The PET image showed localized accumulation of PET tracers in 9L glioma of the rat. |
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