Copper-Mediated Late-Stage Radical Trifluoromethylation of Pyrazole-Type Scaffolds

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Authors: Lucie S. Eisen, Jan H. Griwatz, Sven G. Ruf, María M. Méndez, Enrique Gómez‐Bengoa
Cited by: 1
References: 69

Abstract

High Resolution Image Download MS PowerPoint Slide Trifluoromethylated pyrazoles and their derivatives are of great interest due to their biological and pharmacological relevance. However, efficient methods for their preparation via late-stage trifluoromethylation strategies remain limited. Herein, we report a practical and efficient method for the direct trifluoromethylation of pyrazoles using in situ generated CF 3 radicals and inexpensive copper(II) salts as catalysts at room temperature. The method exhibits excellent functional group tolerance. DFT studies support the observed reactivity trends and provide insight into the electronic effects governing CF 3 radical addition. This strategy holds promise for the generation of highly substituted pyrazoles of interest in biomedical and crop-science applications.

Fields of Study & Subjects

Fluorine in Organic Chemistry Radical Photochemical Reactions Inorganic Fluorides and Related Compounds

Publication details

Journal / source
ACS Omega
Publisher
American Chemical Society (ACS)
Volume
11
Issue
6
Pages
10664–10673
Publication date
4 February 2026
Language
EN