CF₃SO₂Na-Mediated, UV-Light-Induced Friedel–Crafts Alkylation of Indoles with Ketones/Aldehydes and Bioactivities of Products

Abstract

A concise, one-step route to produce 3,3'-diindolylmethanes (DIMs) from simple indoles and ketones or aldehydes is reported. The key step is the ready formation of indole derivatives that involves the in situ conversion of CF₃SO₂Na reagent to ·CF₃ under oxygen or air (1.0 atm) and UV irradiation. It is disclosed that most of the obtained DIMs show anticancer activities in human bladder cancer cell lines EJ and T24.