Department of Chemistry, Indian Institute of Technology Guwahati, 781039, India.
Org Biomol Chem. 2019 Feb 13;17(7):1800-1804. doi: 10.1039/c8ob02309c.
An unprecedented method for the direct arylation and heteroarylation of tetrahydroisoquinolines under metal and oxidant free conditions is reported. The arylation reactions occurred via a C(sp3)-H functionalization enabled three component condensation of tetrahydroisoquinolines, 9-fluorenone imine, and arenes without involving a pre-functionalization/pre-derivatization step. A wide range of arenes and heteroarenes participated in the reaction to provide structurally diverse arylated tetrahydroisoquinolines with good to excellent yields.
报告了一种在无金属和氧化剂条件下直接芳基化和杂芳基化四氢异喹啉的空前方法。芳基化反应通过 C(sp3)-H 官能化实现，三组分缩合四氢异喹啉、9-芴酮亚胺和芳烃，无需涉及预官能化/预衍生化步骤。广泛的芳烃和杂芳烃参与反应，提供了具有良好至优异收率的结构多样的芳基化四氢异喹啉。
