Specific Synthesis of 3H‑Indole Derivatives via Rh(III)-Catalyzed Cascade Annulation between N‑Phenylbenzimidamides and Pyridotriazoles

An efficient synthetic method to construct 3H-indole derivatives has been successfully developed involving rhodium-catalyzed highly selective C–H bond activation of N-phenylbenzimidamides and subsequent couplings with pyridotriazoles. This cascade approach features excellent chemoselectivity and unique of products containing quaternary carbon center with the pyridyl moiety.本研究成功开发了一种高效构建3H-吲哚衍生物的合成方法，该方法通过铑催化N-苯基苯甲脒（N-phenylbenzimidamides）的高选择性C-H键活化（C–H bond activation），并与吡啶并三唑（pyridotriazoles）进行后续偶联反应得以实现。该级联反应策略展现出优异的化学选择性（chemoselectivity），所得产物均带有连有吡啶基片段（pyridyl moiety）的季碳中心（quaternary carbon center），结构独特。