Rh-Catalyzed Construction of Quinolin-2(1H)‑ones via C–H Bond Activation of Simple Anilines with CO and Alkynes

A novel and efficient Rh-catalyzed
carbonylation and annulation
of simple anilines with CO and alkynes through N–H and C–H
bond activation for the direct synthesis of quinolin-2­(1H)-ones has been developed. Simple anilines without preactivation,
broad substrate scope with hetero/polycycles, and high-value products
make this protocol very practical and attractive. A key rhodacycle
complex was isolated and well-characterized.

本研究开发了一种新颖且高效的钯催化的羰基化与环合反应，该反应以CO和炔烃为原料，通过N-H和C-H键的活化，直接合成喹啉-2-(1H)-酮。该方案无需预活化即可应用于简单的芳胺，具有广泛的底物范围，特别是对于含有杂环或多环的底物，同时能够生产高附加值产品，使其在合成化学领域极具实用性和吸引力。研究人员成功分离并详细表征了一个关键的钯催化循环复合物。