The preparation of phthalazinone derivatives is pivotal for their utilization as pharmaceutical agents and other entities. Herein, we report the phthalazinone-assisted carbon–nitrogen bond forming reaction using dioxazolones as robust amidation sources under Rh­(III) catalysis. The broad functional group tolerance and complete site-selectivity are observed. Notably, a series of transformations of synthesized compounds into biologically relevant N-heterocycles demonstrates the applicability of the developed methodology.

Ruthenium(II)-catalyzed C(sp 2 )−H functionalization of N-aryl phthalazinones with a range of aldehydes and activated ketone is described. Initial formation of hydroxyalkylated phthalazinones and subsequent Mitsunobu cyclization provided facile access to biologically relevant indazolophthalazinones. The utility of this method is highlighted by synthetic transformations into a series of potentially bioactive scaffolds.

The facile synthesis of hydroxymethylated indole derivatives is crucial for their further development as pharmaceutical compounds and other synthetic purposes. Herein, we describe the ruthenium­(II)-catalyzed hydroxymethylation of indolines and other N-heterocycles using paraformaldehyde as an abundant C1 feedstock. A wide substrate scope range and high levels of site selectivity as well as functional group tolerance were observed.

The ruthenium(II)-catalyzed cross-coupling reaction between 2-aryl quinazolinones and activated aldehydes is described. The method enables the site‐selective hydroxyalkylation under redox-neutral conditions. Moreover, this protocol provides a facile access to various...

The site‐selective modifications of quinazolinones constitute a pivotal topic in drug discovery and material science. Herein, we describe the rhodium(III)‐catalyzed C–H amidation of 2‐aryl quinazolin‐4(3H)‐ones with a range of nitrene surrogates including dioxazolones, organic azides, and N‐methoxyamides. Complete site‐selectivity and functional group tolerance are observed. Notably, the large‐scale reaction and late‐stage functionalization highlight the synthetic potential of the developed protocol. Combined mechanistic investigations elucidate a plausible reaction mechanism of this process.

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The Cover Feature shows the rhodium(III) and iridium(III)‐catalyzed C–H amidation reaction of 2‐aryl quinazolin‐4(3H)‐ones with a range of nitrene surrogates including dioxazolones dioxazolones, organic azides, and N‐methoxyamides through N‐assisted C–H activation. Complete site‐selectivity and functional group tolerance are observed. Notably, the large‐scale reaction and late‐stage functionalization highlight the synthetic potential of the developed protocol. This work is dedicated to Prof. Pierre H. Dixneuf for his outstanding contribution to organometallic chemistry and catalysis. More information can be found in the Full Paper by S. Hong, I. S. Kim et al.

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