Copper-Catalyzed Three-Component Annulations of Alkenes, Nitrosoarenes, and N-Hydroxyallylamines To Form Fused Oxazinane/Isoxazolidine Heterocycles.

Rahul Kisan Kawade, Rai-Shung Liu
Author Information
  1. Rahul Kisan Kawade: Department of Chemistry, National Tsing-Hua University, Hsinchu, Taiwan.
  2. Rai-Shung Liu: Department of Chemistry, National Tsing-Hua University, Hsinchu, Taiwan.

Abstract

One-pot cascade annulations among nitrosoarenes, alkenes, and N-hydroxyallylamines have been achieved with CuCl/O catalysts, forming fused oxazinane/isoxazolidine heterocycles with excellent diastereoselectivity (d.r. >20:1). To enhance the synthetic utility, we developed a successive cleavage of the two N-O bonds of the resulting heterocycles. A mechanism involving dipolar [3+2] cycloadditions of nitrone intermediates with their tethered alkenes is postulated for formation of these heterocycles.

Keywords

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