Copper-catalyzed acylation of pyrazolones with aldehydes to afford 4-acylpyrazolones

Abstract

Copper-catalyzed direct acylation of the alkenyl C–H bond in 1,2-dihydro-3H-pyrazol-3-ones has been developed, affording a series of 4-acylpyrazolones in moderate to good yields. Notably, this protocol involves readily accessible substrates and reagents, which have good functional group tolerance leading to pyrazolone derivatives under mild reaction conditions.