Siméon Fabrice G, Culligan William J, Lu Shuiyu, Pike Victor W
Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892-1003, USA.
Molecules. 2017 May 12;22(5):792. doi: 10.3390/molecules22050792.
Pd(0)-mediated coupling between iodoarenes, [C]carbon monoxide and aryltributylstannanes has been used to prepare simple model [C]aryl ketones. Here, we aimed to label four 2-aminoethylbenzofuran chemotype based molecules ([C]-) in the carbonyl position, as prospective positron emission tomography (PET) radioligands for the histamine subtype 3 receptor (H3R) by adapting this methodology with use of aryltrimethylstannanes. Radiosynthesis was successfully performed on a platform equipped with a mini-autoclave and a liquid handling robotic arm, within a lead-shielded hot-cell. Candidate radioligands were readily formulated in saline containing ethanol (10%, /) and ascorbic acid (0.5 mg/10 mL). Yields for preclinical use were in the range of 5-9%, decay-corrected from cyclotron-produced [C]CO₂ and molar activities were >115 GBq/µmol at end of synthesis. Radiochemical purities exceeded >97%.
钯（0）介导的碘代芳烃、一氧化碳与芳基三丁基锡之间的偶联反应已被用于制备简单的模型芳基酮。在此，我们旨在通过采用芳基三甲基锡，对该方法进行改进，在羰基位置标记四种基于2-氨基乙基苯并呋喃化学类型的分子（[C] - ），作为组胺3型受体（H3R）的正电子发射断层扫描（PET）放射性配体。在配备微型高压釜和液体处理机器人手臂的平台上，在铅屏蔽热室中成功进行了放射性合成。候选放射性配体很容易在含有乙醇（10%，/）和抗坏血酸（0.5 mg/10 mL）的盐水中配制。临床前使用的产率在5 - 9%范围内，由回旋加速器产生的[C]CO₂进行衰变校正，合成结束时的摩尔活度>115 GBq/µmol。放射化学纯度超过>97%。
