Synthesis of a new fluorine-18-labeled bexarotene analogue for PET imaging of retinoid X receptor |
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| Institution: | 1. Department of Radiology, Keio University School of Medicine, Tokyo, Japan;2. Department of Radiology, Tokyo Medical Center, National Hospital Organization, Tokyo, Japan;3. Department of Urology, Tokyo Medical Center, National Hospital Organization, Tokyo, Japan;1. Department of Applied Chemistry, Graduate School of Engineering, Osaka Prefecture University, 1-1 Gakuen-cho, Nakaku, Sakai, Osaka 599-8531, Japan;2. Department of Bioscience and Informatics, Graduate School of Life and Environmental Science, Osaka Prefecture University, 1-1 Gakuen-cho, Nakaku, Sakai, Osaka 599-8531, Japan |
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| Abstract: | The reference standard 2-fluoro-4-(1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)vinyl)benzoic acid was synthesized from 2,5-dimethyl-2,5-hexanediol and 2-fluoro-4-methylbenzoic acid in 10 steps with 3% overall chemical yield. The precursor 2-nitro-4-(1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)vinyl)benzoic acid was synthesized from 2,5-dimethyl-2,5-hexanediol and dimethyl-2-nitroterephthalate in seven steps with 2% overall chemical yield. The target tracer 2-18F]fluoro-4-(1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)vinyl)benzoic acid was synthesized from its nitro-precursor by the nucleophilic substitution with K18F]F/Kryptofix 2.2.2 and isolated by HPLC combined with solid-phase extraction (SPE) purification in 20–30% radiochemical yield with 37–370 GBq/μmol specific activity at end of bombardment (EOB). |
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| Keywords: | Bexarotene Retinoid X receptor (RXR) Apolipoprotein E (APOE) Positron emission tomography (PET) Alzheimer’s disease (AD) Cancer |
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