LAUSR

Abstract Isoxazole is an important pharmacophore that is critical for biological activity. The isoxazole ring ranks 33rd in frequency among the 351 ring systems found in marketed drugs, thus suggesting a great deal of interest in the synthesis of functional isoxazoles. In recent years, various approaches have been developed for the synthesis and functionalization of isoxazoles. This comprehensive survey summarizes the recent new synthetic approaches to functionalized isoxazoles, with particular focus on the last three years with regard to the following reaction types: (1) 1,3-dipolar cycloaddition, (2) condensation, (3) cycloisomerization, and (4) direct functionalization.