Expedient Synthesis of Pyrroloquinolinones by Rh-Catalyzed Annulation of N‑Carbamoyl Indolines with Alkynes through a Directed C–H Functionalization/C–N Cleavage Sequence

A Rh-catalyzed redox-neutral C–H functionalization of N-carbamoyl indolines with various internal alkynes has been developed. The reaction, which involves the sequential cleavage of the C–H bond of the indoline at the C7-position and the C–N bond of the urea motif, provides a divergent protocol to rapidly assemble fused-ring pyrrolo­quinolinone analogues by using a direct alkenylation/annulation strategy with high efficiency and selectivity.本研究开发了一种铑（Rh）催化的氧化还原中性N-氨基甲酰基二氢吲哚与多种内炔烃的C-H官能化反应。该反应通过依次断裂二氢吲哚C7位的C-H键与脲基的C-N键，采用直接烯基化/环化策略，可快速构建稠合吡咯并喹啉酮类似物，具有高反应效率与选择性。