Department of Chemistry, University of Chicago, Chicago, IL 60637, USA.
Department of Applied Chemistry, China Agricultural University, 2 West Yuanmingyuan Road, Beijing, 100193, China.
Angew Chem Int Ed Engl. 2018 Mar 26;57(14):3815-3819. doi: 10.1002/anie.201800958. Epub 2018 Mar 5.
A direct and catalytic method is reported here for β-arylation of N-protected lactams with simple aryl iodides. The transformation is enabled by merging soft enolization of lactams, palladium-catalyzed desaturation, Ar-X bond activation, and aryl conjugate addition. The reaction is operated under mild reaction conditions, is scalable, and is chemoselective. Application of this method to concise syntheses of pharmaceutically relevant compounds is demonstrated.
本文报道了一种 N-保护的内酰胺与简单芳基碘化物的β-芳基化的直接和催化方法。该转化通过合并内酰胺的软烯醇化、钯催化的去饱和、Ar-X 键活化和芳基共轭加成来实现。反应在温和的反应条件下进行，可规模化，并具有化学选择性。该方法在药物相关化合物的简洁合成中的应用得到了证明。
