Journal
ORGANIC LETTERS
Volume 18, Issue 10, Pages 2427-2430Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.6b00949
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Funding
- National Natural Science Foundation of China [21425415, 21274058]
- National Basic Research Program of China [2015CB856303]
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A versatile, traceless C-H activation-based approach for the synthesis of diversified heterocycles is reported. Rh(III)-catalyzed, N-amino-directed C-H alkenylation generates either olefination products or indoles (in situ annulation) in an atom- and step-economic manner at room temperature. The remarkable reactivity endowed by this directing group enables scale-up of the reaction to a 10 g scale at a very low catalyst loading (0.01 mol %/0.1 mol %). Ex situ annulation of olefination product provides entry into an array of heterocycles.
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