Synthesis of Novel Heterocycles by Amide Activation and Umpolung Cyclization

Org Lett. 2020 Mar 20;22(6):2376-2380. doi: 10.1021/acs.orglett.0c00571. Epub 2020 Mar 11.

Abstract

Herein, we report a metal-free synthesis of cyclic amidines, oxazines, and an oxazinone under mild conditions by electrophilic amide activation. This strategy features an unusual Umpolung cyclization mode and enables the smooth union of α-aryl amides and diverse alkylazides, effectively rerouting our previously reported α-amination transform.

Publication types

  • Research Support, Non-U.S. Gov't