Search

Alkynes generally serve as C2 synthons in transition‐metal‐catalyzed C−H annulations, herein, exploiting electron‐deficient alkynes as unconventional C1 synthons, the chemo‐ and regiospecific synthesis of functionalized 1H‐imidazo[1,5‐a]indol‐3(2H)‐ones via a redox‐neutral rhodium(III)‐catalyzed [4+1] annulation of N‐carbamoyl indoles has been achieved. This process is characterized by high chemo‐ and regioselectivity, broad substrate scope, good tolerance of functional groups, moderate to high yields and mild redox‐neutral conditions, thus affording a robust approach to access valuable 1H‐imidazo[1,5‐a]indol‐3(2H)‐ones. [ABSTRACT FROM AUTHOR]

The metal‐free selective and diverse synthesis of three distinct sets of isoindolinones from 2‐alkynylbenzoic acids and amines has been achieved in a reaction‐condition‐controlled manner. This method exhibits valuable advantageous features such as available starting materials, broad substrate scope, excellent selectivity, good to high yields, good functional group tolerance, simple operation, high bond‐forming efficiency, and step economy, thus providing a convenient and efficient access to a variety of heterocyclic compounds incorporating the bioactive isoindolinone motif. [ABSTRACT FROM AUTHOR]