Fluorine and Iodine Reagents for Asymmetric Synthesis of Biologically Active Molecules
This community develops chemical methods to introduce fluorine and iodine into organic molecules, creating stable building blocks for pharmaceuticals, agrochemicals, and molecular imaging agents.
The work centers on the synthesis of fluorinated and iodinated derivatives, with a strong emphasis on stereoselective and enantioselective reactions. Key methodologies include hypervalent iodine(III) reagents, nucleophilic fluorination, and photoredox or metal-catalyzed cross-coupling of unactivated alkenes. Recurring substrates include carboxylic acids, amino acids, and gem-difluoroalkenes, often processed into trifluoromethylated or gem-difluorinated products. These reactions aim to produce chiral building blocks and functionalized intermediates that enhance the metabolic stability and biological activity of small molecules, supporting applications in drug discovery and radiopharmaceuticals.
The community is most heavily represented in fluorine research, accounting for 5.0% of all tracked fluorine papers, and iodine research, comprising 2.6% of that element’s output. Fluorine also contributes the highest absolute number of papers within this group, with 9,034 entries.
The group comprises 31,062 papers, published primarily in the Journal of Fluorine Chemistry, The Journal of Organic Chemistry, and Organic Letters.
Recent work focuses on the metabolic stability of fluorinated small molecules, the use of halogens in FDA-approved drugs, and regioselective functionalization of fluorinated alkenes and cyclopropanes.