Enantioselective Reaction of 2 H-Azirines with Oxazol-5-(4 H)-ones Catalyzed by Cinchona Alkaloid Sulfonamide Catalysts

Org Lett. 2021 Mar 19;23(6):2104-2108. doi: 10.1021/acs.orglett.1c00259. Epub 2021 Mar 2.

Abstract

The enantioselective reaction of 2H-azirines with oxazol-5-(4H)-ones (oxazolones) using a cinchona alkaloid sulfonamide catalyst has been developed. The reaction proceeded at the C-2 position of oxazolones to afford products with consecutive tetrasubstituted stereogenic centers in high yield with high diastereo- and enantioselectivity. The obtained aziridines were converted into various chiral compounds without loss of enantiopurity.

Publication types

  • Research Support, Non-U.S. Gov't