Synthesis and application of haloisoxazoles

Copper Nanoparticles on Montmorillonite K-10: A Versatile Catalyst for the One-Pot Synthesis of 3,5-Disubstituted Isoxazoles Using Various Methodologies

“…The isoxazole ring can be accessed through various synthetic strategies (Figure 2 ), with the 1,3-dipolar cycloaddition between alkynes and nitrile oxides being the most commonly employed route. 7a Other frequently used methods for constructing the isoxazole ring include condensation of hydroxylamine with 1,3-diketones or α,β-unsaturated ketones, 7b cycloisomerization of ynone oximes 7c and direct functionalization of isoxazoles. 7d…”

Two‐stage Regioselective Access to Non‐symmetric 3,5‐Diarylisoxazoles: Synthesis of Combretastatin A‐4 analogues

“…[4] In terms of selective functionalization of isoxazole ring, including arylation, transition-metal-catalyzed cross-coupling reactions are of great synthetic importance and haloisoxazoles, as the initials for these transformations, constitute an extremely useful group of molecules. [5] Cross-coupling reactions of haloisoxazoles are also interesting because they open a convenient approach to the creation of combinatorial libraries of new heterocyclic compounds, as well as make it possible to speed up the lead optimization process in structure-activity relationship studies in searching for new drugs. [6] The value of isoxazole scaffold for medicinal chemistry and drug discovery, as well as the progress in this field prompted us to develop a new synthetic methodology for the regioselective preparation of 3,5-diarylisoxazoles of non-symmetric structure.…”