Metal-Free Insertion Reactions of Diazo Carbonyls to Azlactones

J Org Chem. 2018 Sep 21;83(18):11399-11406. doi: 10.1021/acs.joc.8b01683. Epub 2018 Aug 31.

Abstract

Insertion reactions of diazo carbonyls to azlactones in basic conditions have been performed. The developed method allows the preparation of a wide range of oxazole derivatives in yields ranging from 74 to 98%. Different substituents on both azlactone rings and diazo carbonyls do not compromise the methodology, even those containing stereogenic centers. Isotopic labeling experiments revealed the mechanism may proceed through a rare diazo carbonyl activation by an ammonium salt derivative.

Publication types

  • Research Support, Non-U.S. Gov't