Palladium-catalyzed ?-arylation Reaction Of Carbonyl Derivatives

In recent years,with the development of organometallic chemistry,transition metal-catalyzed ?-arylation of carbonyl derivatives with aryl halides or pseudohalides had become one of the important methods for the formation of carbon-carbon bonds,and even it had been a hot topic in the field of organometallic chemistry.Reaction mechanism was mainly through oxidative addition,reductive elimination.With the design and utilization of different kinds of phosphine ligands and aza carbene ligands,the scope of substrates were expanded greatly,and the arylation was widely applied in the synthesis of natural products and pharmaceutical active molecules.1.Arylation of a-heterosubstituted cyclic ketone was first studied in the second chapter.The optimal condition was determined after scanning the solvents,bases,catalysts and ligands.Reaction proceeded efficiently in the toluene at 100? with 5 mol%Pd(dba)2 as catalyst,NaOt-Bu as base,6 mol%quinine as ligand.The yields of ?-arylated products were achievd from 50%to 92%.2.The intramolecular arylation of 2-oxindole to afford spirooxindole was first developed in the third chapter.Yields of the products were up to 93%in the presence of 5 mol%Pd(OAc)2 as catalyst,6 mol%t-Bu3P·HBF4 as ligand,and NaOt-Bu as base in THF solvent.