Selectfluor-Triggered Tandem Cyclization of o-Hydroxyarylenaminones To Access Difluorinated 2-Amino-Substituted Chromanones

J Org Chem. 2017 Sep 15;82(18):9837-9843. doi: 10.1021/acs.joc.7b01339. Epub 2017 Aug 25.

Abstract

A practical and straightforward synthetic route through a Selectfluor-triggered tandem cyclization of o-hydroxyarylenaminone was developed to construct a variety of difluorinated 2-amino-substituted chromanones. This novel protocol features mild reaction conditions, operational simplicity, and broad substrate scope. The enamine moiety in o-hydroxyarylenaminone played dual roles to enable high efficiency in the difluorination and intramolecular cyclization, leading to the accomplishment of a new class of difluorinated 2-amino-substituted chromanones for pharmaceutical studies.

Publication types

  • Research Support, Non-U.S. Gov't