Synthesis of 1,2-Dihydro-Substituted Aniline Analogues Involving N-Phenyl-3-aza-Cope Rearrangement Using a Metal-Free Catalytic Approach

Abstract EN

An efficient metal-free domino reaction leading to structural/electronically divergent 1,2-dihydropyridines from easily accessible propargyl vinyl anilines via N-phenyl 3-aza-Cope sigmatropic rearrangement is reported with good to excellent yields using 1,2-dichlorobenzene as solvent under thermal conditions.

Spirocyclic substitution is also tolerated under the present optimized conditions.