Utilizing tertiary alkylamines as reliable two-carbon building blocks, a concise and efficient route for the regioselective synthesis of biquinolines from 2-methylquinolines and arylamines has been established. This I₂-promoted approach enables a [4π + 2σ] annulation of three nucleophilic species via two kinds of transient enamines. The C(sp³)–H annulation strategy is also extended to other methylazaarenes toward constructing nonsymmetrical benzo[f]quinoline-containing biheteroaryls. Notably, the applicability of this process for the late-stage functionalization of complex molecules highlights its considerable potential for application in biorelevant areas.

中文翻译：

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I2 促进三种不同胺的氧化环化以获得不同的双杂芳基


利用叔烷基胺作为可靠的双碳结构单元，已经建立了一种从 2-甲基喹啉和芳胺区域选择性合成双喹啉的简洁有效的路线。这种 I₂ 促进的方法通过两种瞬时烯胺实现了三种亲核物种的 [4π + 2σ] 环化。C（sp³）-H 环化策略也扩展到其他甲基氮杂芳烃，以构建非对称的含苯并 [f] 喹啉的双杂芳基。值得注意的是，该工艺对复杂分子后期功能化的适用性突出了其在生物相关领域应用的巨大潜力。