Visible Light-Promoted Three-Component Reaction for the Synthesis of Pyrrolopyrazoles

作者：Han‐Peng Pan, Shao‐Shuai Chen, Han Yang, Zhanhao Su, Yajie Chen, Mao-Bi Zhu, Ai‐Jun Ma, Xiang‐Zhi Zhang · 发表于：Organic Letters · 年份：2025 · DOI：10.1021/acs.orglett.5c00896 · 被引用次数：11 · 研究领域：Oxidative Organic Chemistry Reactions、Radical Photochemical Reactions、Catalytic C–H Functionalization Methods

A visible light-enabled three-component cascade assembles pyrrolopyrazoles from arylalkynes, benzoquinones, and 5-aminopyrazole through a mechanistically validated carbonyl-alkyne metathesis/(3 + 2)-cycloaddition/1,2-aryl migration sequence. This protocol delivers pyrrolopyrazole heterocycles in up to 96% yield with excellent functional group tolerance. Preliminary biological screening identified promising antitumor activity in selected products, highlighting the potential value of this method. The proposed reaction mechanism is supported by control experiments.