Dedicated to Prof. S. Chandrasekaran: New Synthetic Methods and Strategies in Organic
Synthesis.
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.
Keywords
Intramolecular oximation - HFIP -
O-Propargyl hydroxylamine - Isoxazoline - One-pot synthesis - Luciferase inhibitors