Herein, we reported a one-pot synthesis of N-CF3 diarylamines using AgSCF3 and AgF. This work provides a robust protocol for the efficient trifluoromethylation modification of diarylamines, enabling the concise one-pot synthesis of diarylamines bearing a pharmaceutically privileged N-CF3 unit while demonstrating excellent functional group tolerance and steric hindrance compatibility. The obtained diaryl N-CF3 compounds were subjected to biological evaluation, and the results revealed that N-CF3 derivative 2y exhibits good in vitro anti-lung carcinoma activities.
Zhang et al. (Mon,) studied this question.