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Copper-Catalyzed Trifluoromethylation of Unactivated Olefins

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TLDR
A recent surge in the number of reports describing the formation of carbon-trifluoromethyl (C-CF3) bonds, demonstrating the continuing need for the development of efficient methods to incorporate these groups as discussed by the authors.
Abstract
The inclusion of fluorinated functional groups in small molecules has had a profound impact on the pharmaceutical, material, and agrochemical industries.[1, 2] In particular, the trifluoromethyl (CF3) substituent has emerged as an important functional group for the modulation of the physical properties in new pharmaceutical candidates as it has excellent metabolic stability, lipophilicity, and is electron-withdrawing in nature.[3] Myriad of fluorinated biologically active pharmaceutical compounds have been identified,[4] with an estimated 20% of drugs on the market containing fluorine.[1] On this basis, there has been a recent surge in the number of reports describing the formation of carbon–trifluoromethyl (C–CF3) bonds, demonstrating the continuing need for the development of efficient methods to incorporate these groups.

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Citations
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Introduction of Fluorine and Fluorine-Containing Functional Groups

TL;DR: This Review gives a brief summary of conventional fluorination reactions, including those reactions that introduce fluorinated functional groups, and focuses on modern developments in the field.
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Recent advances in copper-catalyzed dehydrogenative functionalization via a single electron transfer (SET) process.

TL;DR: This tutorial review summarizes the recent advances in the copper-catalyzed dehydrogenative functionalization via a single electron transfer (SET) process achieving C-C, C-N,C-O, c-halogen atoms, N-P, and N-N bond formation.
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Catalysis of Radical Reactions: A Radical Chemistry Perspective.

TL;DR: This work critically address both catalyst-free and catalytic radical reactions through the lens of radical chemistry, using basic principles of kinetics and thermodynamics to address problems of initiation, propagation, and inhibition of radical chains.
References
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Journal ArticleDOI

Fluorine in Pharmaceuticals: Looking Beyond Intuition.

TL;DR: Experimental progress in exploration of the specific influence of carbon-fluorine single bonds on docking interactions is reviewed and complementary analysis based on comprehensive searches in the Cambridge Structural Database and the Protein Data Bank is added.
Journal ArticleDOI

Aromatic Trifluoromethylation with Metal Complexes

TL;DR: Molecules bearing a trifluoromethyl group constitute one of the most important classes of selectively fluorinated compounds, and derivatives bearing the CF3 group on aromatic rings are particularly numerous and important.
BookDOI

Fluorine in medicinal chemistry and chemical biology

Iwao Ojima
TL;DR: This book discusses applications of fluorinated amino acids and peptides to chemical biology and pharmacology, and recent Advances in the Syntheses of Fluorinated Amino Acids.
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