Synthesis of C3-Alkylated Indoles on DNA via Indolyl Alcohol Formation Followed by Metal-Free Transfer Hydrogenation

Org Lett. 2019 Sep 6;21(17):6633-6637. doi: 10.1021/acs.orglett.9b02132. Epub 2019 Aug 14.

Abstract

3-Alkylated indole cores have been found in countless natural products and many biologically active compounds, including pharmaceuticals. In this report, a highly efficient approach to C3-alkylated indole derivatives on DNA via indolyl alcohol formation followed by metal-free transfer hydrogenation is developed. This on-DNA C3 alkylation approach is attractive because library compounds can be constructed from simple aldehydes or acid functionalized aldehydes, which are widely commercially available.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alcohols / chemistry*
  • Alkylation
  • DNA / chemistry*
  • Hydrogenation
  • Indoles / chemical synthesis*
  • Indoles / chemistry
  • Molecular Structure

Substances

  • Alcohols
  • Indoles
  • DNA