CuI-catalyzed cascade cyclization using indole-3-carbaldehydes and amidines for the synthesis of
Yanjun Xie1, Yi Liang1, Xinbo Liu1
1Key Laboratory for Environmental Catalysis & Waste Regeneration of Hunan Province, College of Materials and Chemical Engineering, Hunan Institute of Engineering, Xiangtan 411104, P. R. China. Yanjun-Xie@hnie.edu.cn.
Abstract:
We report a copper-catalyzed cascade cyclization for the concise synthesis of pyrimido[4,5-b]indole skeletons via direct C-H functionalization and concomitant C-N bond formation. This methodology utilizes an inexpensive catalytic system (CuI/2,2'-bipyridine). The reaction demonstrates remarkable functional group tolerance and consistently delivers the target heterocycles in good to excellent yields. The insights gained from our studies are expected to advance general efforts towards the efficient synthesis of biology-oriented privileged heterocyclic skeletons.
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