Transition-metal-free intramolecular double hydrofunctionalization of alkyne to access 6/7/5-fused heterocyclic skeletons

Abstract

We describe a novel intramolecular double hydrofunctionalization cyclization of alkyne with nitrogen and oxygen nucleophilic groups to construct valuable 6/7/5-fused heterocyclic products. This post-Groebke–Blackburn–Bienaymé (GBB) reaction introduces a new class of functionalized isocyanides. Transition-metal-free cyclization, broad substrate scope, and high atom economy were some features of the present protocol.