University of Oxford, Chemistry Research Laboratory, 12 Mansfield Road, Oxford, OX1 3TA, UK.
Chem Soc Rev. 2018 Sep 17;47(18):6990-7005. doi: 10.1039/c8cs00499d.
Radiolabelled (bio)molecules have advanced many areas of science from fundamental biology to human health including applications in molecular imaging and more generally nuclear medicine. Today, the field of radiochemistry is rapidly expanding, a trend resulting from the increasing demand for labelled molecules necessary for diagnosis and to accelerate pharmaceutical drug development. More often, the synthesis of labelled (bio)molecules employs a pre-functionalised precursor to allow for the chemoselective installation of a particular radioisotope-containing substituent. Among the array of precursors available, boron reagents occupy a prominent place because they are easy to handle, numerous possibilities exist for their preparation, and their reactivity has been well studied especially in cross-coupling chemistry. In this review, we discuss the value of boron-based precursors for the radiolabelling of (bio)molecules with the radionuclides carbon-11, fluorine-18, iodine-123, iodine-125 and iodine-131, and we illustrate how these radiosynthetic advances have opened the radiochemical space available for areas such as PET and SPECT imaging.
放射性标记（生物）分子已经推动了从基础生物学到人类健康的许多科学领域的发展，包括在分子成像和更广泛的核医学中的应用。如今，放射化学领域正在迅速发展，这一趋势是由于对用于诊断和加速药物开发的标记分子的需求不断增加所致。更常见的是，标记（生物）分子的合成采用预官能化的前体，以允许对特定含有放射性同位素的取代基进行化学选择性安装。在可用的众多前体中，硼试剂占有突出的地位，因为它们易于处理，有多种方法可以制备，并且它们的反应性已经得到了很好的研究，特别是在交叉偶联化学中。在这篇综述中，我们讨论了基于硼的前体在使用放射性核素碳-11、氟-18、碘-123、碘-125 和碘-131 对（生物）分子进行放射性标记方面的价值，并说明了这些放射合成方面的进展如何为 PET 和 SPECT 成像等领域开辟了可用的放射化学空间。
