Base-Promoted ß-C(sp(3))-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 ß-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.