Hypervalent Iodine(III)-Mediated Umpolung Dialkoxylation of N-Substituted Indoles

J Org Chem. 2022 Oct 7;87(19):12759-12771. doi: 10.1021/acs.joc.2c01326. Epub 2022 Sep 28.

Abstract

Herein, we report dialkoxylation of N-substituted indoles through a hypervalent iodine-mediated umpolung strategy, affording trans-2,3-dimethoxyindolines with up to 95% yield. In addition, C5-selective bromination of 2,3-dialkoxyindoline via NBS-mediated rearomatization was achieved. DFT calculation of the sequence of electrophilic addition and nucleophilic substitution pathway of N-substituted indoles has also been investigated.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Indoles
  • Iodides
  • Iodine*

Substances

  • Indoles
  • Iodides
  • Iodine