Trifluoroethanol promoted formal nucleophilic substitution of indol-2-yl diaryl methanol for the synthesis of tetraarylmethanes.
Cuicui NianRun YuZhengyu HanYang BaiJianhao WangJianwei SunJun Yong KangPublished in: Chemical communications (Cambridge, England) (2024)
The synthesis of tetraarylmethanes has long been a challenge in the field of synthetic chemistry. In this study, a series of tetraarylmethanes were successfully synthesized through the formal nucleophilic substitution reaction of indol-2-yl diaryl methanol catalyzed by Brønsted acid. The key success of this study lies in suppressing the influence of water molecules by forming hydrogen bonds with the TFE solvent. This process leads to the formation of active 2-indole imine methide (2-IIM) intermediates, ensuring the successful synthesis of tetraarylmethanes. Furthermore, some of the products also exhibited potential anticancer activity.