An expedient synthesis of oxazepino and oxazocino quinazolines

Abstract

A synthetic route to a new class of privileged tri- and tetra-cyclic quinazolines containing a medium-sized ring is reported. An expedient synthetic route involving nucleophilic aromatic substitution, and sequential Niementowski and BOP-mediated ring closures afforded a collection of analogues. The scope of the reaction was explored in terms of cyclic and acyclic linkers, ring size and substitution pattern.