Palladium-catalyzed alpha-arylation of indolin-3-ones

Abstract

A method for the catalytic alpha-arylation of indolin-3-ones was developed. The catalytic system comprising Pd(dba)(2) and PAd(3) was found to be optimal for the transformation. The protocol features broad functional group compatibility in that a range of arylated indoxyl derivatives bearing a fully substituted carbon center was synthesized with high efficiency. A preliminary bioassay study revealed that the selected indole-substituted indolin-3-ones exhibit favorable cytotoxic activities against HCT-116 cancer cell line.