Asymmetric Total Synthesis of Eburnamine and Eucophylline: A Biomimetic Attempt for the Total Synthesis of Leucophyllidine

Org Lett. 2017 Jun 16;19(12):3267-3270. doi: 10.1021/acs.orglett.7b01410. Epub 2017 Jun 1.

Abstract

The first enantiospecific total synthesis of (+)-6 has been achieved employing a Friedländer quinoline synthesis as a key step. Asymmetric synthesis of the architecturally complex eburnamine 5 has also been accomplished utilizing an intramolecular acid-mediated cyclization of a carbinol amine lactone moiety. Highlights of the effective modular synthetic strategy include development of the common precursor 4 for the construction of the privileged scaffolds 5 and 6 with an all-carbon quaternary stereocenter utilizing a Johnson-Claisen rearrangement strategy. Attempts have been made to synthesize 1 by the biomimetic coupling of 5 and (+)-6; however, regioisomeric 26 was formed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Azabicyclo Compounds / chemistry*
  • Biomimetics
  • Cyclization
  • Indole Alkaloids
  • Molecular Structure
  • Stereoisomerism

Substances

  • Azabicyclo Compounds
  • Indole Alkaloids
  • eucophylline
  • leucophyllidine