Here, we established optimized conditions for a mild ¹⁸F‐fluorination to yield ¹⁸F‐deprenyl and ¹⁸F‐D₂‐deprenyl as neuroinflammation imaging agents by fully automatic synthesis. Initially, manual synthesis with 1 mg of precursor and pH = 7.8 KOMs elution buffer yielded 85–92% of ¹⁸F‐incorporation yields and showed nondecay corrected yields of 15–17%. Fully automatic synthesis showed a nondecay corrected radiochemical yield of 10.7 ± 0.46%. Owing to low precursor input, the maximum molar activity achieved was 1302.4 ± 26.4 GBq/μmol. Our mild ¹⁸F‐fluorination procedure showed higher radiochemical yields and molar activity than those by previously used procedures, even with minimized precursor input.

中文翻译：

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轻度18F氟化和最小前体输入量用于神经炎症的PET成像，优化18F‐D2-Depenyl的合成

在这里，我们建立了温和的¹⁸ F-氟化条件，以通过全自动合成产生¹⁸ F-去异戊烯基和¹⁸ F-D _2-去异戊烯基作为神经炎症显像剂的优化条件。最初，使用1 mg前体和pH = 7.8 KOMs洗脱缓冲液进行人工合成，可得到¹⁸ F掺入量的85–92％，并显示15-17％的非衰减校正产率。全自动合成显示未经衰减校正的放射化学产率为10.7±0.46％。由于前体输入量低，因此获得的最大摩尔活性为1302.4±26.4 GBq /μmol。我们的温和¹⁸F-氟化程序显示出比以前使用的程序更高的放射化学产率和摩尔活性，即使前体输入量最少。