Mild and general method for the alpha-arylation of heteroaromatic ketones.
The development of a general and mild method for Pd-catalyzed alpha-arylation of a variety of ketones bearing multiple heteroatoms is described. The ligand to metal ratio and the position of the heteroatoms with respect to the carbonyl moiety significantly impact the efficiency of these transformations. In addition, these conditions were successfully applied to the alpha-arylation of cyclic imines. A detailed investigation of the scope of this methodology, including the effect of the ligand to metal ratio, is discussed.
Bristol-Myers Squibb, 1 Squibb Drive, New Brunswick, New Jersey 08903, USA. lopa.desai@bms.com
Lopa V
LV
Desai
Danan T
DT
Ren
Thorsten
T
Rosner
D002384:Catalysis; D006863:Hydrogen-Ion Concentration; D007659:Ketones / Q000737:chemistry*; D008024:Ligands; D010165:Palladium / Q000737:chemistry
D007659:Ketones; D008024:Ligands; D010165:Palladium