A Strategy for Amide to β-Oxo Ester Transformation via N-Alkenoxypyridinium Salts as the Activator and H2O as the Nucleophile

Org Lett. 2020 Sep 18;22(18):7118-7122. doi: 10.1021/acs.orglett.0c02457. Epub 2020 Sep 2.

Abstract

N-Alkenoxypyridinium salts were found to be highly active electrophilic reagents that could be used to activate the C-N bond of amides. Both aromatic amides and aliphatic amides could be transformed into the corresponding β-oxo esters with good yields via the combined use of N-alkenoxypyridinium salts and water. The methodology proceeds under mild reaction conditions and is tolerant of various functional groups in both reaction partners.

Publication types

  • Research Support, Non-U.S. Gov't