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Facilitate the development of bioactive molecules
Recently, researchers from the Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, have made new progress in the study of aromatics trifluoromethylation
.
They used photo-redox catalysis combined with aryl sulfoxide to provide a new way for the generation of trifluoromethyl radicals, which are expected to be applied to the later modification of natural products and drug molecules, and help the development of biologically active molecules
Fluorine is the most electronegative element with a small atomic radius.
The introduction of fluorine atoms or fluorine-containing groups into drug molecules can improve the membrane permeability, metabolic stability and bioavailability of drug molecules
.
Trifluoromethyl is one of the common fluorine-containing groups in drug molecules, and most of them are in the aromatic structure
From the perspectives of atom economy, reagent cost, and ease of operation, trifluoroacetic acid is an ideal source of trifluoromethyl
.
However, due to its extremely high oxidation potential, it needs to be converted into trifluoroacetic acid radicals under severe conditions such as strong oxidants, high temperature heating or ultraviolet radiation, and then release carbon dioxide to generate trifluoromethyl radicals
