Non-natural 2 H -azirine-2-carboxylic acids: an expedient synthesis and antimicrobial activity.
Pavel A SakharovAlexander N KoronatovAlexander F KhlebnikovMikhail S NovikovArtem G GlukharevElizaveta V RogachevaLiudmila A KraevaVladimir V SharoykoTatiana B TennikovaNikolai V RostovskiiPublished in: RSC advances (2019)
Non-natural 2 H -azirine-2-carboxylic acids were obtained in high yields by FeCl 2 -catalyzed isomerization of 5-chloroisoxazoles to azirine-2-carbonyl chlorides followed by their hydrolysis. The 3-aryl- and 3-heteroaryl-substituted acids are stable during prolonged storage, exhibit antibacterial activity against ESKAPE pathogens and show a low level of cytotoxicity.