This method shows efficient access to tetrahydropyrido[1,2-a]indol-6-one derivatives with high diastereoselectivity, indicating its broad substrate scope and metal-free conditions.
Tetrahydropyrido[1,2-a]indol-6-one is a significant motif that is widely present in natural bioactive alkaloids. Herein, a facile and efficient access to the tetrahydropyrido[1,2-a]indol-6-one skeleton via NHC (N-heterocyclic carbene)-catalyzed radical relay dearomatization of indoles has been developed. This protocol exhibits metal-free, mild reaction conditions, a broad substrate scope, high efficiency, and excellent diastereoselectivity (30 examples, up to 89% yield and >20:1 dr).
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Huang et al. (2025) studied this question.
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