The ruthenium(II)‐catalyzed CH carbonylation of 2‐aryl quinazolinones with isocyanates as carbonyl sources is described. The developed method provides direct access to biologically relevant isoindoloquinazolinone core through CH aminocarbonylation followed by intramolecular annulation. A broad range of substrate scope and functional group tolerance were observed. Gram‐scale reactions and synthetic transformations demonstrate the synthetic potential of this protocol.
The development of new methods for the direct synthesis of bioactive molecules is a pivotal topic in organic and medicinal chemistry. Herein, we describe the rhodium (III)-catalyzed CÀ H functionalization of N-aryl phthalazinones with maleimides. The complete site-selectivity and broad functional group tolerance are observed. Notably, this protocol allows the direct integration of phthalazinones and succinimides, which are vital motifs found in bioactive natural products and pharmaceuticals.
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