分会

第十二分会：元素/金属有机

摘要

Alkylamines are an important class of compounds in organic synthesis and medicinal chemistry.[1] The enrichment of three-dimensional architectures and the degrees of saturation is a fundamental strategy to expand the structural complexities of alkylamines,[2-4] thereby expediting the development of biologically active molecules and active pharmaceutical ingredients. Classic alkylamine synthesis may suffer from low availability or inaccessibility of aliphatic coupling partners, significantly limiting the available scope of alkylamine entities. While photocatalytic two-component reactions have become versatile strategies to broaden the chemical space of alkylamines, the multicomponent amination version remains underdeveloped. Here, we describe a metallaphotoredox-promoted three-component amination method using tertiary alkylamines, nitroarenes, and carboxylic acids as economic and broad-scope reaction substrates. This chemo- and regioselective transformation encompasses the formal amine group transposition and C–H alkylation of tertiary alkylamines, providing a modular and streamlined strategy to offer architecturally diverse and functionalized N-alkyl anilines for organic synthesis and drug discovery.

关键词

metallophotoredox, multicomponent reactions, C-N coupling, nitroarenes, anilines

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