Synthesis of fluorinated oxygen- and sulfur-containing heteroaromatics

• Syntheses of fluorinated oxygen- and sulfur-containing heteroaromatics are reviewed.
• Both direct and indirect methods for preparing fluorinated rings are described.
• Nucleophilic and electrophilic sources of fluorine are compared.

The incorporation of fluorine into a target molecule may have a considerable impact on its reactivity, selectivity, biological activity and physical properties. This is especially true in medicinal chemistry where fluorine is often employed as a bioisostere of hydrogen and where many important drug compounds also feature heteroaromatic rings. This work complements existing reviews on the synthesis of fluorinated, aromatic heterocycles, with a focus on less common oxygen-containing heteroaromatics as well as their sulfur-based analogues.

This review covers methods for the incorporation of fluorine into oxygen- and sulfur-containing heteroaromatic compounds.Figure optionsDownload as PowerPoint slide