One‐Pot Synthesis of 3,5‐Disubstituted Isoxazoles from Propargylic Alcohols through Propargylic <i>N</i>‐Hydroxylamines

Abstract

Abstract An efficient approach has been described for the synthesis of 3,5‐disubstituted isoxazoles from propargylic alcohols. The strategy involves a one‐pot p ‐TSA‐catalyzed N ‐propargylation of protected hydroxylamines followed by a TBAF‐mediated detosylative 5‐ endo ‐ dig cyclization. The method was successfully used for the synthesis of various 3,5‐disubstituted isoxazoles.