Boron reagents for divergent radiochemistry,Chemical Society Reviews

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Boron reagents for divergent radiochemistry
Chemical Society Reviews ( IF 40.4 ) Pub Date : 2018-08-24 00:00:00 , DOI: 10.1039/c8cs00499d
Thomas C. Wilson _{1,

2,

3,

4} , Thomas Cailly _{5,

6,

7,

8,

9} , Véronique Gouverneur _{1,

2,

3,

4}

Affiliation

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.

中文翻译：

用于发散放射化学的硼试剂

从基础生物学到人类健康，放射性标记（生物）分子已在许多科学领域取得了进步，包括分子成像和更广泛的核医学应用。如今，放射化学领域正在迅速扩展，这一趋势是由于对诊断和加速药物开发所必需的标记分子的需求不断增加所致。更经常地，标记的（生物）分子的合成采用预官能化的前体，以允许化学选择性地安装特定的含放射性同位素的取代基。在一系列可用的前体中，硼试剂占有优势地位，因为它们易于处理，其制备存在多种可能性，并且对它们的反应性进行了深入研究，尤其是在交叉偶联化学中。在这篇评论中，

更新日期：2018-08-24

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