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.
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Dongke Zhang
Xinru Zhai
Y. Z. Zhou
Organic Letters
Nankai University
State Key Laboratory of Chemical Engineering
State Key Laboratory of Medicinal Chemical Biology
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Zhang et al. (Mon,) studied this question.
www.synapsesocial.com/papers/6996a7ffecb39a600b3ee4e8 — DOI: https://doi.org/10.1021/acs.orglett.5c05447