Abstract
A sequential copper‐catalyzed Sonogashira coupling followed by an intramolecular hydroamination and palladium‐catalyzed intramolecular direct arylation reaction was developed to provide a convenient and modular approach for the synthesis of useful azepino‐fused isoindolinones. Nineteen azepino‐fused isoindolinones were prepared in moderate to high (22–90 %) yields. The developed protocol tolerated various functional groups and involved the formation of one carbon–nitrogen and two carbon–carbon bonds in a one‐pot fashion. The palladium‐catalyzed intramolecular direct arylation step involved formation of an unusual eight‐membered palladacycle.
Published Version
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