Synthesis of α-Fluoro-α-nitroarylacetates via Vicarious Nucleophilic Substitution of Hydrogen

J Org Chem. 2016 Dec 2;81(23):11751-11757. doi: 10.1021/acs.joc.6b02219. Epub 2016 Nov 7.

Abstract

Readily available ethyl chlorofluoroacetate, when treated with a strong base, forms an α-chloro-α-fluorocarbanion that adds to nitroarenes at a position ortho or para to the nitro group with formation of anionic σH adducts. Subsequent base-induced β-elimination of HCl proceeds selectively to give nitrobenzylic α-fluorocarbanions and, upon protonation, ethyl α-fluoro-α-nitroarylacetates.

Publication types

  • Research Support, Non-U.S. Gov't