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.

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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
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Synthesis and Biological Evaluation of N–CF 3 Diaryl Amines

Y. Z. Zhou, Zijian Li, Yulong Li, Dongke Zhang et al.
Organic Letters
Fluorine in Organic Chemistry
article

Synthesis and Biological Evaluation of N–CF 3 Diaryl Amines

Y. Z. Zhou, Zijian Li, Yulong Li, Dongke Zhang, Xinru Zhai, Changliang Shan, Qian Wu
article en

Abstract

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.

Organic LettersVol. 28(8)
Nankai University (CN), State Key Laboratory of Chemical Engineering (CN), State Key Laboratory of Medicinal Chemical Biology
Good health and well-being
Openalex Percentile: Top 53%
Fluorine in Organic Chemistry
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