School of Chemistry, University of Bristol , Bristol BS8 1TS, United Kingdom.
J Am Chem Soc. 2017 Oct 11;139(40):14005-14008. doi: 10.1021/jacs.7b07830. Epub 2017 Sep 27.
We outline a simple protocol that accesses directly unprotected secondary amines by intramolecular C-N bond forming dearomatization or aryl C-H amination. The method is dependent on the generation of a potent electrophilic aminating agent released by in situ deprotection of O-Ts activated N-Boc hydroxylamines.
我们提出了一种简单的方案,可以通过分子内 C-N 键形成去芳构化或芳基 C-H 胺化来直接访问未保护的仲胺。该方法依赖于原位脱保护 O-Ts 活化的 N-Boc 羟胺生成的强亲电胺化剂。