Innovative approaches to the synthesis of five-membered heteroaromatics with emerging synthetic methodologies

Abstract

According to statistics, more than 70% of drugs that are available on the market contain heterocyclic units. Among them, five-membered heteroaromatics bearing nitrogen, oxygen, and sulfur have served as the most important structural motifs found in diverse pharmaceuticals. Emerging toolboxes, such as photocatalysis, biocatalysis, electrocatalysis and skeletal editing have showcased unprecedented avenues to access them. In fact, >300 publications on the topic of synthesis of five-membered heteroaromatics by using emerging toolboxes have been recorded in the last ten years, clearly indicating the significance of this field. In this study, a conceptual overview and discussions are presented to showcase the advancement of this field. Moreover, the related drugs and bioactive compounds obtained by these approaches are highlighted.