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

Tianbao Yang, Huiai Lu, Yixuan Shu, Yifeng Ou, Ling Hong, Chak-Tong Au, Renhua Qiu

Organic letters 2020 Feb 07

filter terms:

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.

Citation

Tianbao Yang, Huiai Lu, Yixuan Shu, Yifeng Ou, Ling Hong, Chak-Tong Au, Renhua Qiu. CF3SO2Na-Mediated, UV-Light-Induced Friedel-Crafts Alkylation of Indoles with Ketones/Aldehydes and Bioactivities of Products. Organic letters. 2020 Feb 07;22(3):827-831