Department of Chemistry, Kangwon National University, Chuncheon 200-701, Korea.
Org Lett. 2015 Apr 17;17(8):1830-3. doi: 10.1021/acs.orglett.5b00625. Epub 2015 Apr 1.
C-N-coupled heterobiaryls were synthesized by sequential N-H functionalization reactions: stereoselective rhodium-catalyzed N-H insertion, followed by regioselective palladium-catalyzed C-H amination. Because of the good substrate scope and excellent selectivity, the developed method presents a novel approach for the synthesis of heterobiaryls, which are potent antibiotics.
通过顺序的 N-H 官能化反应合成 C-N 偶联的杂芳基：立体选择性的铑催化的 N-H 插入，接着是区域选择性的钯催化的 C-H 胺化。由于良好的底物范围和优异的选择性，所开发的方法为合成具有强效抗生素作用的杂芳基提供了一种新途径。
