We present a method for synthesizing -benzyl pyridones from -quinone methides (-QMs) and 2- or 4-hydroxy pyridines in the presence of a base at room temperature. The reaction proceeds through 1,6-Michael addition reaction. Simple operation, good to excellent yields, broad substrate scope, and good functional group tolerance are the salient features of the developed methodology. The synthesized -benzyl pyridones displayed significant blood-stage antiplasmodial activity at sub-micromolar concentration.

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http://dx.doi.org/10.1039/d4ob01686fDOI Listing

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