Minisci-Photoredox-Mediated α-Heteroarylation of N-Protected Secondary Amines: Remarkable Selectivity of Azetidines
Minisci-Photoredox-Mediated α-Heteroarylation of N-Protected Secondary Amines: Remarkable Selectivity of Azetidines
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DOI：
10.1021/acs.orglett.8b00991
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发表时间：
2018-10-05
期刊：
影响因子：
5.2
通讯作者：
Berthelot, Didier
中科院分区：
文献类型：
--
作者：
Bosset, Cyril;Beucher, Helene;Berthelot, Didier
报道了在Minisci介导的光氧化还原条件下，通过与N-保护胺（包括氮杂环丁烷）的C-H官能化，对N-杂芳烃进行一般的、温和的和官能团耐受的直接官能化。探索了广泛的取代氮杂环丁烷，包括螺环衍生物和杂环。该反应使得能够在一个步骤中从未活化的原料胺和杂环制备富含sp3的复杂药物样结构。
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.