Synthesis of 4-Hetarylisoxazoles from Amino Acid-Derived Halogenoximes and Push-Pull Enamines
Eur. J. Org. Chem. 2018, 40, 5585-5595
An approach to 4‐hetarylisoxazole‐derived amines and other related 3,4‐disubstituted isoxazoles which relies on [3+2] cycloaddition of amino acid‐derived halogenoximes and push‐pull enamines is described. The target products are obtained at gram scale in up to 81 % overall yield. The efficiency of the method is affected by the electronic properties of the enamine component at the key step.