[carbonyl-C]Benzyl acetate: automated radiosynthesis via Pd-mediated [C]carbon monoxide chemistry and PET measurement of brain uptake in monkey

[羰基-C]苄基乙酸酯:通过钯介导的[C]一氧化碳化学实现自动化放射合成,并利用PET测量猴脑摄取

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Abstract

[carbonyl-(11)C]Benzyl acetate ([(11)C]1) has been proposed as a potential agent for imaging glial metabolism of acetate to glutamate and glutamine with positron emission tomography (PET). [(11)C]1 was synthesized from [(11)C]carbon monoxide, iodomethane and benzyl alcohol via palladium-mediated chemistry. The radiosynthesis was automated with a modified Synthia platform controlled with in-house developed Labview software. Under production conditions, [(11)C]1 was obtained in 10% (n = 6) decay-corrected radiochemical yield from [(11)C]carbon monoxide in > 96% radiochemical purity and with an average specific radioactivity of 2,415 mCi/micromol. The total radiosynthesis time was about 45 min. Peak uptake of radioactivity in brain (SUV = 3.1) was relatively high and may be amenable to measuring uptake and metabolism of acetate in glial cells of the brain.

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