Thermally induced formal [4+2] cycloaddition of 3-aminocyclobutenones with electron-deficient alkynes: facile and efficient synthesis of 4-pyridones

Abstract

A thermally induced novel formal [4+2] cycloaddition of cyclobutenones with electron-deficient alkynes under metal-free conditions has been developed for the first time. The reaction can proceed in a highly regioselective manner and provides a straightforward and efficient method for the synthesis of 4-pyridone derivatives from readily available starting materials in a single step.