Jian Rong

The radical fluoroalkylation of isocyanides with fluorinated sulfones is enabled by visible-light photoredox catalysis. A wide range of readily available mono-, di-, and trifluoromethyl heteroaryl sulfones can thus be used as efficient radical fluoroalkylation reagents under mild conditions. This method not only describes a new synthetic application of fluorinated sulfones, but also provides a new route to fluoroalkyl radicals.

Sonnige Aussichten: Durch die im Titel beschriebene Sequenz werden 2-(3,4-Dihydroisochinolin-2(1H)-yl)essigsäureethylester mit einer Reihe elektronenarmer Alkene und Alkine effizient in Pyrrolo[2,1-a]isochinoline umgewandelt (siehe Schema; bpy=2,2′-Bipyridin, EWG = elektronenziehende Gruppe). Die Reaktion bietet eine neue Strategie zum direkten Aufbau der Kernstruktur natürlicher Lamellarin-Alkaloide. Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.

Abstract Positron emission tomography (PET) is a molecular imaging technology that provides quantitative information about function and metabolism in biological processes in vivo for disease diagnosis and therapy assessment. The broad application and rapid advances of PET has led to an increased demand for new radiochemical methods to synthesize highly specific molecules bearing positron‐emitting radionuclides. This Review provides an overview of commonly used labeling reactions through examples of clinically relevant PET tracers and highlights the most recent developments and breakthroughs over the past decade, with a focus on 11 C, 18 F, 13 N, and 15 O.

Abstract Owing to the excellent performance of fluorinated compounds in the areas of pharmaceuticals, agrochemicals, and materials chemistry, organic chemists have made great efforts towards the selective incorporation of fluorine or fluorinated moieties into organic molecules through nucleophilic, electrophilic, radical, and metal‐catalyzed pathways. Impressive progress in fluorination and perfluoroalkylation (especially trifluoromethylation) reactions has been made over the past few decades. However, methods for incorporating lightly fluorinated groups (such as −CF 2 H) are still underdeveloped, in spite of their important applications in pharmaceuticals and agrochemicals. This Focus Review summarizes recent developments in metal‐catalyzed direct difluoromethylation reactions.

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.