Highly Selective Synthesis of α-Aminoamide Utilizing an Umpolung Reaction and Characteristics of α-Hydrazonoester

Org Lett. 2021 Jun 4;23(11):4168-4172. doi: 10.1021/acs.orglett.1c01117. Epub 2021 May 20.

Abstract

An umpolung reaction with α-hydrazonoesters was investigated, and it was found that α-N,N-dialkylaminoamides could be directly synthesized in yields up to 92% via a concomitant rearrangement of dialkylamino groups. As an application, a short synthesis of an inhibitor of glycine type-1-transporter was accomplished via subsequent functional group transformations in 28% overall yield.

Publication types

  • Research Support, Non-U.S. Gov't