铑(Ⅲ)催化吲哚甲酰胺衍生物与末端炔烃的C—H活化/环化反应

Rhodium(Ⅲ)-Catalyzed C—H Activation/Cylization of Indole-2-amides Derivatives and Terminal Alkynes

报道了铑（Ⅲ）催化的吲哚甲酰胺衍生物与末端的炔烃发生的C—H活化/环化反应,能够高效地构建多环吲哚类化合物,收率为85%~98%.该反应操作简便、反应条件温和、催化剂用量低,并使用具有氧化性的导向基团,不需要添加额外氧化剂.研究了该反应的分子间的竞争性试验,推测了可能的反应机理.所有化合物均采用NMR,IR,高分辨质谱等多种谱学技术进行了结构表征.

A simple and efficient Rh-catalyzed the C—H activation/cyclization reaction of indole-2-amides and alkynes was developed. A series of novel pyrido[3,4-b]indol-1-ones can be efficiently obtained with high to excellent yields using the internal oxidant at room temperature. The transformations have a wide range of substrates with various functional groups. Intermolecular competition experiment was conducted, and a plausible mechanism was proposed. The structures of all conpound were confirmed by 1H NMR, 13 C NMR and HRMS.