Concise and high-yield synthesis of T808 and T808P for radiosynthesis of [18F]-T808, a PET tau tracer for Alzheimer’s disease |
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| Institution: | 1. Department of Cardiovascular Medicine, Kyushu University Hospital, Fukuoka, Japan;2. Sleep Apnea Center, Kyushu University Hospital, Fukuoka, Japan;3. Department of Cardiovascular Medicine, Saiseikai Futsukaichi Hospital, Fukuoka, Japan;4. Clinical Physiological Laboratory, Saiseikai Futsukaichi Hospital, Fukuoka, Japan;1. Université de Strasbourg, IPHC, 23 rue du Loess, 67037 Strasbourg, France;2. CNRS, UMR 7178, 67037 Strasbourg, France |
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| Abstract: | The authentic standard T808 and its corresponding mesylate precursor T808P were synthesized in six steps using ethyl vinyl ether and trichlorocetyl chloride as starting materials. The overall chemical yields of T808 and T808P were 35% and 52%, respectively. 18F]-T808 was synthesized from T808P by the nucleophilic substitution with K18F]F/Kryptofix 2.2.2 and isolated by HPLC combined with solid-phase extraction (SPE) purification in 35–45% radiochemical yield with 37–370 GBq/μmol specific activity at end of bombardment (EOB). |
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| Keywords: | Tau tracer Automation Positron emission tomography (PET) Alzheimer’s disease (AD) |
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