A Broad Substrate Scope of Aza-Friedel-Crafts Alkylation for the Synthesis of Quaternary α-Amino Esters

Org Lett. 2020 Aug 7;22(15):5822-5827. doi: 10.1021/acs.orglett.0c01895. Epub 2020 Jul 10.

Abstract

A versatile synthetic protocol of aza-Friedel-Crafts alkylation has been developed for the synthesis of quaternary α-amino esters. This operationally simple alkylation proceeds under ambient conditions with high efficiency, regioselectivity, and an exceptionally broad scope of arene nucleophiles. A key feature of this alkylation is the role associated with the silver(I) salt counteranions liberated during the reaction. Taking advantage of a phase-transfer counteranion/Brønsted acid pair mechanism, we also report a catalytic enantioselective example of the reaction.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Alkylation*
  • Catalysis
  • Esters / chemistry*
  • Molecular Structure
  • Stereoisomerism

Substances

  • Esters