4.8 Article

Minisci-Photoredox-Mediated alpha-Heteroarylation of N-Protected Secondary Amines: Remarkable Selectivity of Azetidines

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ORGANIC LETTERS
卷 20, 期 19, 页码 6003-6006

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AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.8b00991

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The development of a general, mild, and functional-group-tolerant direct functionalization of N-heteroarenes by C-H functionalization with N-protected amines, including azetidines under Minisci-mediated photoredox conditions, is reported. A broad scope of substituted azetidines, including spirocyclic derivatives, and heterocycles were explored. This reaction enables the production of sp3-rich complex druglike structures in one step from unactivated feedstock amines and heterocycles.

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