A new synthesis of 2-deoxy-2-[18f]fluoro-D-galactose using [18f]fluoride ion |
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Authors: | Terushi Haradahira Minoru Maeda Yasunobu Kai Masaharu Kojima |
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Institution: | Faculty of Pharmaceutical Sciences, Kyushu University Maidashi 3–1–1, Higashi-ku, Fukuoka 812, Japan |
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Abstract: | A nucleophilic radiofluorination of methyl 3,4-0-isopropylidene-2-0-(trifluoromethanesulfonyl)-6-0-trityl-β-D- talopyranoside ( 1 ) with aminopolyether (Kryptofix 2.2.2.) supported potassium 18F]fluoride in acetonitrile gave methyl 2-deoxy-2-(18F) fluoro-3,4-o-isopropylidene-6-0-trityl-β-D-galactopyranoside ( 2 ). Hydrolysis of 2 with 6N HCl followed by passage through an ion retardation resin column and a neutral alumina column gave 2-deoxy-2-18F]fluoro-D-galactose (2-18FDGal) in 36–39% overall radiochemical yield without correction for decay. The total preparation time was about 90 min from start of the radiofluorination. |
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Keywords: | radiofluorination no-carrier-added methyl 3 4-0-isopropylidene-2-0-(trifluoromethanesulfonyl)-6-0-trityl-β-D- talopyranoside 2-deoxy-2-[18F] fluoro-D-galactose |
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