A short, novel approach to 2,3,4a,5-tetrahydro-1H-pyrazino[1,2-a] quinoline-4,6-diones
An expeditious route to constrained arylpiperazinones has been developed. The key reaction formed the tricyclic system in one-pot via a 1,4-addition-lactamization-aromatic substitution sequence. Four examples were prepared.