Recent Advances in the Synthesis and Applications of Oxaborole Derivatives

Abstract

Oxaboroles, five-membered boron-containing heterocycles, have emerged as an increasingly versatile framework in drug discovery and molecular design. Their significance stems from the unique Lewis acidity of the boron center, which enables reversible covalent interactions with biological targets. This property has led to the successful development of FDA-approved therapeutics such as tavaborole (antifungal) and crisaborole (anti-inflammatory), sparking widespread research interest. This review comprehensively summarizes the key advancements in the synthesis and application of oxaborole derivatives over the last decade. The synthetic methodologies are systematically categorized based on the principal starting materials, including alkynes, alkenes, aryl halides, aryl boronic acids, and oxaboranes. Emphasis is placed on the development of sustainable and efficient routes, such as photocatalytic, mechanochemical, and continuous-flow processes. Along with the synthesis, the review also covers the expanding applications of these compounds in different fields.