Solbach C, Uebele M, Reischl G, Machulla H-J
Radiopharmacy, PET-Center, University Hospital Tübingen, Roentgenweg 15, D-72076 Tübingen, Germany.
Appl Radiat Isot. 2005 Apr;62(4):591-5. doi: 10.1016/j.apradiso.2004.09.003.
The synthesis of carbon-11 amino function labelled uncharged Thioflavin T derivatives is known to be performed by reaction of the demethyl-precursors with [11C]methyl iodide but the labelling yields are only mediocre. The use of [11C]methyl triflate improved the radiochemical yield of three potential beta-amyloid imaging PET-radiotracers significantly. Performance of the labelling reaction by reacting the corresponding precursor molecules with [11C]methyl triflate for 1 min at 80 degrees C led to radiochemical yields of 44+/-10% (n=5) for [11C]6-Me-BTA-1, 68+/-4% (n=10) for [11C]BTA-1 and 58+/-2% (n=5) for [11C]6-OH-BTA-1 with respect to [11C]methyl triflate. In production runs (60 min, 50 microA) up to 6500 MBq (mean: 4000+/-1900 MBq) of [11C]6-Me-BTA-1, 7900 MBq (mean: 6000+/-1000 MBq) of [11C]BTA-1 and 7100 MBq (mean: 6300+/-600 MBq) of [11C]6-OH-BTA-1 could be obtained ready for intravenous injection. The radiochemical purity was >95% with specific activities in the range of 80-120 GBq/micromol (EOS) within a total synthesis time of less than 40 min after EOB.
已知碳-11氨基功能标记的不带电荷的硫黄素T衍生物的合成是通过脱甲基前体与[11C]甲基碘反应进行的，但标记产率仅为中等水平。使用[11C]甲基三氟甲磺酸酯显著提高了三种潜在的β-淀粉样蛋白成像PET放射性示踪剂的放射化学产率。通过使相应的前体分子与[11C]甲基三氟甲磺酸酯在80℃下反应1分钟进行标记反应，相对于[11C]甲基三氟甲磺酸酯，[11C]6-Me-BTA-1的放射化学产率为44±10%（n = 5），[11C]BTA-1的放射化学产率为68±4%（n = 10），[11C]6-OH-BTA-1的放射化学产率为58±2%（n = 5）。在生产运行（60分钟，50微安）中，可获得高达6500 MBq（平均：4000±1900 MBq）的[11C]6-Me-BTA-1、7900 MBq（平均：6000±1000 MBq）的[11C]BTA-1和7100 MBq（平均：6300±600 MBq）的[11C]6-OH-BTA-1，可供静脉注射。放射化学纯度>95%，比活度在80 - 120 GBq/μmol（EOS）范围内，在EOB后总合成时间少于40分钟。
