Rapid entry into heterocycle-fused benzylic azepines and azocines via directed metallation/ring-closing metathesis

Abstract

The efficient synthesis of a range of heterocycle-fused benzylic azepine and azocine derivatives is reported, employing a directed metallation/ruthenium-catalysed ring-closing metathesis approach. A base-mediated tautomerisation approach can be used to access both the azepine and azocine derivatives from the same starting material.