Synthesis and Biological Evaluation of N–CF <sub>3</sub> Diaryl Amines
Herein, we reported a one-pot synthesis of N-CF<sub>3</sub> diarylamines using AgSCF<sub>3</sub> 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-CF<sub>3</sub> unit while demonstrating excellent functional group tolerance and steric hindrance compatibility. The obtained diaryl N-CF<sub>3</sub> compounds were subjected to biological evaluation, and the results revealed that N-CF<sub>3</sub> derivative <b>2y</b> exhibits good <i>in vitro</i> anti-lung carcinoma activities.
Authors
- Y. Z. Zhou
- Zijian Li (ORCID: https://orcid.org/0000-0002-9291-5966)
- Yulong Li
- Dongke Zhang
- Xinru Zhai
- Changliang Shan
- Qian Wu
Institutions
- Nankai University (CN)
- State Key Laboratory of Chemical Engineering (CN)
- State Key Laboratory of Medicinal Chemical Biology
Publication Details
- Journal
- Organic Letters
- Published
- 2026-02-16
- DOI
- https://doi.org/10.1021/acs.orglett.5c05447
- Primary Topic
- Fluorine in Organic Chemistry
- Type
- article
- Field-Weighted Citation Impact
- 0.00