Organocatalyzed Multicomponent Synthesis of Isoxazolidin-5-ones

Org Lett. 2015 Nov 6;17(21):5408-11. doi: 10.1021/acs.orglett.5b02755. Epub 2015 Oct 21.

Abstract

An unprecedented multicomponent organocatalyzed Knoevenagel-aza-Michael-cyclocondensation reaction between Meldrum's acid, hydroxylamines, and aldehydes afforded a straightforward entry to a large array of racemic and syn-diastereoenriched isoxazolidinones as synthetically useful scaffolds. This process revealed a markedly facile aza-Michael-cyclocondensation sequence as a key domino reaction between RCO2NHOH and transient alkylidene Meldrum's acid upon Brønsted base catalysis.

Publication types

  • Research Support, Non-U.S. Gov't