College of Chemistry, Zhengzhou University, Zhengzhou, Henan Province 450001, China.
Org Biomol Chem. 2020 May 6;18(17):3312-3323. doi: 10.1039/d0ob00433b.
An I2-mediated synthesis of phenanthridines via intramolecular sp3 C-H amination of readily accessible aniline precursors is reported. The present synthetic process is straightforward and applicable to a broad variety of unprotected aniline substrates, and provides facile and efficient access to phenanthridine derivatives. This C-H amination protocol does not use transition metals, is operationally simple, and can be achieved on a gram scale.
本文报道了一种通过易于获得的苯胺前体的分子内 sp3 C-H 胺化反应实现 I2 介导的菲啶合成方法。本合成过程简单直接,适用于多种未保护的苯胺底物,为菲啶衍生物提供了简便高效的合成途径。该 C-H 胺化反应不使用过渡金属,操作简单,可在克级规模上进行。