Practical route to 2-quinolinones via a Pd-catalyzed C-H bond activation/C-C bond formation/cyclization cascade reaction.

Quinolinone derivatives were constructed via a Pd-catalyzed C-H bond activation/C-C bond formation/cyclization cascade process with simple anilines as the substrates. This finding provides a practical procedure for the synthesis of quinolinone-containing alkaloids and drug molecules. The utility of this method was demonstrated by a formal synthesis of Tipifarnib.

Palladium catalyzed stereoselective C-glycosylation of glycals with enol triflates.

An efficient palladium catalyzed C-glycosylation of glycals with enol triflates has been established. The coupling reactions took place on the anomeric carbon, and the coupling products gave exclusively α isomers. The flexibility of the reaction was exemplified by the broad spectra of substrate scope, constituted of glycals protected with good leaving groups as well as an assortment of enol triflates.