State Key Laboratory of Elemento-Organic Chemistry, Research Institute of Elemento-Organic Chemistry, College of Chemistry , Nankai University , Tianjin 300071 , People's Republic of China.
Collaborative Innovation Center of Chemical Science and Engineering (Tianjin) , Tianjin 300071 , People's Republic of China.
Org Lett. 2018 Sep 21;20(18):5661-5665. doi: 10.1021/acs.orglett.8b02389. Epub 2018 Sep 4.
A photoredox-mediated direct cross-dehydrogenative coupling reaction to accomplish α-aminoalkylation of N-heteroarenes is reported. This mild reaction has a broad substrate scope, offers the first general method for synthesis of aminoalkylated N-heteroarenes without the need for substrate prefunctionalization, and is scalable to the gram level. Furthermore, the reaction was found to be applicable to other hydrogen donors besides amines (i.e., ethers, an aldehyde, a formamide, p-xylene, and alkanes), thus enabling the preparation of N-heteroarenes bearing various types of substituents.
本文报道了一种通过光氧化还原介导的直接交叉脱氢偶联反应实现 N-杂芳基α-氨基烷基化的方法。该温和的反应具有广泛的底物范围，为氨基烷基化 N-杂芳基化合物的合成提供了首例无需底物预官能化的通用方法，并且可扩大到克级规模。此外，该反应还适用于除胺以外的其他氢供体（如醚、醛、甲酰胺、对二甲苯和烷烃），从而能够制备带有各种取代基的 N-杂芳基化合物。
