Related Experiment Video
Updated: Feb 17, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and Biological Evaluation of N-CF3 Diaryl Amines
Dongke Zhang1, Xinru Zhai1, Yi Zhou1
1State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300350, China.
Abstract:
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.
Related Concept Videos
Preparation of 1° Amines: Gabriel Synthesis
Strong bases like NaOH or KOH deprotonate the phthalimide to form the corresponding anion, which acts as a nucleophile. Further, the anion attacks an...
Preparation of 1° Amines: Hofmann and Curtius Rearrangement Overview
Preparation of 1° Amines: Azide Synthesis
Azide ions act as good nucleophiles and react with unhindered alkyl halides to form alkyl azides. Alkyl azides do not participate in further nucleophilic substitution reactions, thereby eliminating the chances of polyalkylated products. Alkyl azides are reduced by hydride-based reducing agents, like lithium aluminum...
Preparation of Amides
The DCC-promoted synthesis of amides begins with the protonation of DCC by carboxylic acid. The protonation makes it a better acceptor. Next, the addition of carboxylate to the protonated carbodiimide gives a reactive acylating agent.
Subsequently, the amine acts as a nucleophile that attacks the acylating agent to form a tetrahedral intermediate. In the...
Preparation of 1° Amines: Hofmann and Curtius Rearrangement Mechanism
Physical Properties of Amines

