Metal-Catalyzed Regiospecific (4+3) Cyclization of 2-Indolylmethanols withortho-Quinone Methides

The first metal-catalyzed C3-nucleophilic (4+3) cyclization of 2-indolylmethanols with stableortho-quinone methides has been established, which constructed indole-based seven-membered heterocycles in high yields (70 %-98 %) with regiospecificity. This reaction has tackled the challenges in exploring the C3-nucleophilicity of 2-indolylmethanols, which will contribute to the chemistry of 2-indolylmethanols, especially to metal-catalyzed cyclizations of 2-indolylmethanols. In addition, this approach will provide a useful method for constructing indole-based seven-membered heterocycles with high efficiency and regioselectivity.