Syntheses of 3-Aryl Tetrahydroisoquinolines via an Intermolecular [4 + 2] Cycloaddition of Sultines with Imines

Org Lett. 2022 Jun 17;24(23):4192-4196. doi: 10.1021/acs.orglett.2c01437. Epub 2022 May 31.

Abstract

The development of an intermolecular aza-Diels-Alder (DA) cycloaddition of sultines and imines is reported. By exploiting sultines as o-quinodimethane precursors and aryl imines as dienophiles in the presence of Cu(OTf)2, an aza-DA reaction proceeds to provide a wide variety of 3-aryl tetrahydroisoquionlines in moderate to excellent yield (up to 89%). The synthetic utility of these products was demonstrated in the preparation of tetracyclic N-heterocycles, including a tetrahydroprotoberberine skeleton.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cyclization
  • Cycloaddition Reaction
  • Imines*
  • Stereoisomerism
  • Tetrahydroisoquinolines*

Substances

  • Imines
  • Tetrahydroisoquinolines