Site-Selective C–H Amidation of 2-Aryl Quinazolinones Using Nitrene Surrogates

作者: Saegun Kim , Daeun Jeoung , Kunyoung Kim , Seok Beom Lee , Suk Hun Lee

DOI: 10.1002/EJOC.202001128

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摘要: 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 …

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