Base-Promoted β-C(sp3)-H Functionalization of Enaminones: An Approach to Polysubstituted Pyridines

A convenient one-pot base-promoted synthesis of polysubstituted pyridines from 1-arylethylamines and ynones through the direct beta-C(sp(3))-H functionalization of enaminones under metal-free conditions has been developed. An intermolecular Michael addition reaction and an intramolecular condensation were involved in this procedure, which features high regioselectivity; high efficiency, and environmental friendliness. Various polysubstituted pyridines were provided in up to 92% yield for 34 examples.