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.

一种基于Rh催化的氧化还原中性C-H官能化反应，该反应针对N-碳酰基吲哚及其内部炔烃的转化，已成功开发。此反应涉及吲哚分子C7位C-H键的连续断裂以及脲基团中C-N键的断裂，从而提供了一种独特的快速构建融合环状吡咯喹啉酮类似物的方案。该方案采用直接烯烃化/闭环策略，具有高效性和高选择性。