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Synthesis of γ-Carboline Derivatives via the Rh(III)-Catalyzed Regioselective C-H Activation/[4+2] Annulation Cascade
Zhangshun Luo1, Yao Chen1, Lijie Lv1
1Basic Medicine Research and Innovation Center for Novel Target and Therapeutic Intervention, Ministry of Education, College of Pharmacy, Chongqing Medical University, Chongqing 400016, China.
Abstract:
Transition-metal-catalyzed annulation represents an attractive approach for constructing diverse bioactive molecules while facing challenges like regioselective control. Herein, an efficient assembly of diverse highly functionalized γ-carboline derivatives from 2H-imidazoles and alkynes has been established. This was achieved through a rhodium(III)-catalyzed C-H activation/[4+2] tandem cyclization cascade, facilitating chemo- and regioselective access to γ-carbolines, which exhibit good anticancer activity, in moderate yields.
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