Palladium-catalyzed direct alkenylation of 4-hydroxy-2-pyridones

The first direct C-3 alkenylation of N -substituted-4-hydroxy-2-pyridones with unactivated alkenes has been achieved under conventional palladium acetate catalysis. The presented protocol enables the efficient production of functionalized furo[3,2- c ]-pyridones-2 when terminal alkenes are utilized and 3-alkenyl-4-hydroxy-2-pyridones when more substituted reaction partners are involved. The mild reaction conditions allow easy, scalable access to pyridone derivatives that resemble core structures isolated from natural alkaloids. The first direct 3-alkenylation of N-substituted 4-hydroxy-2-pyridones with unactivated alkenes is reported through a palladium acetate catalyzed, oxidative coupling.