HFIP-Promoted Intramolecular Oximation of O-Propargyl Hydroxylamines for the Synthesis of 2-Isoxazolines

Abstract A concise and efficient intramolecular oximation enables the rapid and streamlined synthesis of 2-isoxazolines. This metal-free approach offers a broad substrate scope under mild reaction conditions. The successful demonstration of gram-scale and one-pot synthesis highlights both the versatility and scalability of the method. The synthetic utility of this method is further exemplified by converting 2-isoxazolines into β-hydroxy ketones. This method was further used for the synthesis of firefly luciferase inhibitors.