For over a century, aryldiazonium halides have served as widely used building blocks within synthetic chemistry. They are vital intermediates in converting simple anilines to high-value products, incl...

The first general three-component intermolecular Pd-catalyzed carboamination of conjugated enynes enables the coupling of anilines and aryl triflates to produce functionalized allenic amines, utilizi...

#LCSOJournalClub 176.1 (highlighted in picture): This week starts with a photoelectrochemical decarboxylative C-N coupling to access bioisosteres of anilines…

General Characteristics The ortho-acylation of unprotected anilines using nitriles is known as the Sugasawa reaction. The Friedel-Crafts acylation of anilines is inherently difficult because the am…

Preparation of arylsulfonic acids and derivatives can be achieved under mild conditions from aryldiazonium salts, although conventional methods often require isolation or accumulation of these potenti...

The activation of unstrained nonpolar C–C bonds, such as C(aryl)–C(alkyl) bonds, remains challenging to achieve. Existing catalytic strategies predominantly rely on bidentate chelating directing group...

The activation of unstrained nonpolar C–C bonds, such as C(aryl)–C(alkyl) bonds, remains challenging to achieve. Existing catalytic strategies predominantly rely on bidentate chelating directing groups (DGs) or special substrates. Herein, we report a Ru-catalyzed activation of C(aryl)–C(methyl) bonds enabled by a removable mono-DG. By employing a bulky phosphinite or aminophosphine-DG that can be easily installed and removed later, a methyl group at the ortho position of phenols and anilines can be smoothly deleted under the hydrogenolysis condition. This reaction exhibits a broad substrate scope and excellent functional group tolerance. Mechanistic studies suggest that a Ru–hydride species generated in situ is responsible for the C(aryl)–C(methyl) bond activation, with methane identified as a byproduct.

A copper-catalyzed method has been developed for synthesizing β-amino ketones using allyl alcohols and substituted anilines in 2-methyl-THF at 60 °C. This reaction employs hydrogen peroxide (H2O2) as ...

We present a novel copper-catalyzed method for aniline cross-couplings promoted by a 6-hydroxy picolinhydrazide ligand. The method achieves room-temperature reactivity with aryl bromides, enabled by a methanol/ethanol solvent mixture and a mild, functional group-compatible base, with catalyst loadings as low as 0.5 mol %. The use of industrially preferred solvents and base, as well as the high catalytic activity, offers a significant advancement in the practicality and scalability of industrial processes. Furthermore, the approach extends to the cross-coupling of aryl chlorides under elevated temperatures and demonstrates compatibility with additional nucleophile classes.