Access to Benzoxazepines and Fully Substituted Indoles via HDDA Coupling

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.