A facile Horner-Wadsworth-Emmons route to 2-quinolones

2-Quinolones are prepared from o-aminophenylketones by N-acylation with phosphonoalkanoylchlorides, followed by an intramolecular Horner-Wadsworth-Emmons olefination. The transformation proceeds under mild conditions, is generally applicable, gives good yields and can be performed either in two steps or as a one-pot reaction.

2-Quinolones are prepared by an acylation/HWE olefination sequence, which can be performed as a one-pot reaction. This method is applicable to enolisable aminoketones as starting materials. A wide range of substituents are tolerated.