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

Year: 2026
Type: article
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.
Source: ACS Omega
Language: English
Open Access status: gold
Estimated APC paid: $1,935
OpenAlex ID: W7127568258
FWCI: 3.119
Cites: 69
Cited by: 1
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