Allard M, Fouquet E, James D, Szlosek-Pinaud M
Laboratoire d'Imagerie Moléculaire et Fonctionnelle, CNRS-UMR 5231, Université Victor Ségalen Bordeaux 2, Bordeaux, France.
Curr Med Chem. 2008;15(3):235-77. doi: 10.2174/092986708783497292.
Positron Emission Tomography has become a powerful scientific and clinical tool probing biochemical processes in the human body. Their clinical applications have proven to be vital in the evaluation and diagnosis of diseases. This is due, in large part, to advances in instrumentation and synthetic chemistry. Carbon-11 is a valuable radionuclide in PET as it virtually permits the synthesis of radiolabelled versions of any compound of interest. The syntheses with carbon-11 present several features: limited number of labelled precursors, sub-micromolar amounts of the starting materials, and a need for the introduction of the radioisotope as late as possible in the synthesis. All of these reasons have restricted complex radiosyntheses. The short half-life of carbon-11 (20.4 min) requires the rapid preparation and purification of carbon-11 labelled molecules. Those have to be carried out immediately before use from cyclotron produced precursors ([11C]CO2, [11C]CO, [11C]CH4) or reagents rapidly prepared from them ([11C]CH3I, [11C]COCl2, [11C]HCN). As a consequence carbon-11 has been underused compared to fluorine-18. However, because of the increasing molecular complexity and diversity of biologically active compounds, there is a need for new methodologies giving access in short time and high yield to radioactive (11)C-probes. The aim of this review is to emphasize the methodologies used in this field and to give a comprehensive overview of the numerous advances, which occurred over the past decade. In addition, for each labelling technique or reaction reported, a special attention has been brought to classify the applications in function of the targeted medical domain.
正电子发射断层扫描已成为探测人体生化过程的强大科学和临床工具。其临床应用在疾病评估和诊断中已被证明至关重要。这在很大程度上归功于仪器仪表和合成化学的进步。碳 - 11 是正电子发射断层扫描中一种有价值的放射性核素，因为它几乎可以合成任何感兴趣化合物的放射性标记版本。用碳 - 11 进行的合成具有几个特点：标记前体数量有限、起始原料为亚微摩尔量，以及需要在合成过程中尽可能晚地引入放射性同位素。所有这些原因都限制了复杂的放射性合成。碳 - 11 的半衰期短（20.4 分钟），这就要求快速制备和纯化碳 - 11 标记的分子。这些必须在使用前立即从回旋加速器产生的前体（[11C]CO2、[11C]CO、[11C]CH4）或由它们快速制备的试剂（[11C]CH3I、[11C]COCl2、[11C]HCN）中进行。因此，与氟 - 18 相比，碳 - 11 的使用不足。然而，由于生物活性化合物的分子复杂性和多样性不断增加，需要新的方法以便在短时间内高收率地获得放射性（11）C 探针。本综述的目的是强调该领域使用的方法，并全面概述过去十年中出现的众多进展。此外，对于所报道的每种标记技术或反应，都特别关注根据目标医学领域对应用进行分类。
