Palladium-catalyzed α-arylation of indolin-3-ones?

Chemical Communications Pub Date: 2020-03-18 DOI: 10.1039/D0CC00435A

Abstract

A method for the catalytic α-arylation of indolin-3-ones was developed. The catalytic system comprising Pd(dba)2 and PAd3 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.

Graphical abstract: Palladium-catalyzed α-arylation of indolin-3-ones
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