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Published on: November 9, 2019
Pd/NBE-Catalyzed One-Pot Modular Synthesis of Tetrahydro-γ-carbolines
Chuantao Huang1, Wenlin Zhang1, Ying Liu1
1School of Pharmacy, Xianning Medical College, Hubei University of Science and Technology, Xianning 437100, P. R. China.
Abstract:
Tetrahydro-γ-carbolines are especially outstanding fused heterocyclic ring systems possessing significant biological activities in the central nervous system. Here, using commercially available NBE derivatives (NBEs), we report an efficient protocol for the one-pot modular synthesis of 4-substituted tetrahydro-γ-carbolines via Catellani/aza-Michael addition cascade from easily available 3-iodo-1-tosyl-1H-indole, aziridines and olefins. This approach exhibits a wide substrate scope, good yields, scalability, and potential extension toward the synthesis of Mebhydroline analogues.
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