Construction of Fluoro-containing Heterocycles Mediated by Free Radicals

Dynamic Kinetic Resolution-Enabled Highly Stereoselective Nucleophilic Fluoroalkylation to Access Chiral β-Fluoro Amines

“…Amines are privileged structures present in a myriad of biologically active molecules. − However, amino groups typically result in a poor ability to penetrate the cell membrane due to their strong basicity, thus leading to an obvious decrease in the biological activity of drug molecules . Due to the peak electronegativity of fluorine atoms, replacing a C–H bond with a C–F bond can strongly affect the basicity of nearby amino groups. , For example, the p K a value of the protonated 5-HT 1D agonist is 9.7, while that of its β-fluorinated analogue is 8.7 (Figure a). , The change in the p K a value of the drug molecule has an important impact on the kinetic metabolic properties and the affinity, which improves the cell membrane permeability, thereby improving its biological activity. , In addition, fluorine has a considerable effect on the electron distribution of the molecule, while not significantly altering or distorting the general geometry of molecules because of the similar size of hydrogen and fluorine . Thus, ready access to β-fluoro amine is highly desirable and significant for the life sciences and pharmaceutical industry.…”

Recyclable ZnIn2S4 Microspheres for Photocatalytic Azolation of N-Heterocycles

“…The excessive use of fossil energy has caused energy shortage and environmental pollution problems, which can be greatly avoided by the application of renewable solar energy. , Photocatalysis, which converts solar energy into chemical energy, is considered to be a sustainable technology. − Typically, transition metal complexes such as Ru/Ir-based compounds or organic dyes including Eosin Y, Rhodamine, etc., are necessary as photocatalysts for synthetic transformations. − However, these homogeneous photocatalysts could not be reused after the catalytic process. − Therefore, it is preferable to develop sustainable, recyclable, and inexpensive heterogeneous photocatalysts for visible-light-induced organic transformations. − …”

Visible-Light-Promoted Phosphorylation/Cyclization of 1-Acryloyl-2-cyanoindoles in Green Solvent

“…Heterocyclic compounds are abundantly found in synthetic drugs, biologically active products, and pharmaceuticals . Thus, the development of heterocyclic chemistry continues to attract the attention of synthetic organic chemists and medicinal researchers .…”