Positron emission tomography (PET) constitutes a functional imaging technique that is harnessed to probe biological processes in vivo. PET imaging has been used to diagnose and monitor the progression of diseases, as well as to facilitate drug development efforts at both preclinical and clinical stages. The wide applications and rapid development of PET have ultimately led to an increasing demand for new methods in radiochemistry, with the aim to expand the scope of synthons amenable for radiolabeling. In this work, we provide an overview of commonly used chemical transformations for the syntheses of PET tracers in all aspects of radiochemistry, thereby highlighting recent breakthrough discoveries and contemporary challenges in the field. We discuss the use of biologicals for PET imaging and highlight general examples of successful probe discoveries for molecular imaging with PET – with a particular focus on translational and scalable radiochemistry concepts that have been entered to clinical use.

正电子发射断层扫描 (PET) 是一种功能成像技术，用于探测体内生物过程。 PET 成像已用于诊断和监测疾病进展，以及促进临床前和临床阶段的药物开发工作。 PET 的广泛应用和快速发展最终导致对放射化学新方法的需求不断增加，目的是扩大适合放射性标记的合成子的范围。在这项工作中，我们概述了放射化学各个方面合成 PET 示踪剂的常用化学转化，从而突出了该领域最近的突破性发现和当代挑战。我们讨论了生物制品在 PET 成像中的应用，并重点介绍了 PET 分子成像成功探针发现的一般例子，特别关注已进入临床应用的转化和可扩展的放射化学概念。