Access to Benzoxazepines and Fully Substituted Indoles via HDDA Coupling

Org Lett. 2020 Feb 7;22(3):956-959. doi: 10.1021/acs.orglett.9b04499. Epub 2020 Jan 28.

Abstract

The HDDA-derived benzyne intermediate was captured by oxazolines based on the addition reaction of benzyne to the C═N double bond. Benzoxazepine derivatives, fused benzoxazepine derivatives, and fully substituted indoles are synthesized in one step. The reaction does not require any catalyst or additives. Possible reaction mechanisms are presented.

Publication types

  • Research Support, Non-U.S. Gov't