Iridium(III)-Catalyzed C‑7 Selective C–H Alkynylation of Indolines at Room Temperature

An iridium-catalyzed direct C-7 selective C–H alkynylation of indolines at room temperature, for the first time, has been developed via C–H bond activation. Furthermore, the first example of direct C–H alkynylation of carbazoles at the C1 position is also achieved. More importantly, the resulting product can be readily transformed into C7-alkynylated indoles, further widening the C-7 derivatization of indoles and highlighting the synthetic utility of this methodology.本研究首次通过C-H键活化策略，开发出室温条件下铱催化的吲哚啉C-7位选择性直接C-H炔基化反应。此外，本研究还首次实现了咔唑C1位的直接C-H炔基化反应。更为重要的是，所得产物可便捷转化为C7位炔基化吲哚，进一步拓宽了吲哚的C-7位衍生化途径，凸显了该方法学的合成应用价值。