A concise total synthesis of (+)-scholarisine A empowered by a unique C-H arylation

J Am Chem Soc. 2013 Sep 4;135(35):12964-7. doi: 10.1021/ja406546k. Epub 2013 Aug 21.

Abstract

The structurally unique akuammiline alkaloid (+)-scholarisine A was synthesized in 14 steps from a known enone (15 steps from commercial materials) through a route empowered by a unique C-H arylation reaction to forge its polycyclic core. Additional key steps include a pyrone Diels-Alder reaction and a radical cyclization/Keck allylation to fashion the core cage polycycle and one of the molecule's quaternary centers, as well as the use of a carefully positioned pendant hydroxyl group to facilitate the chemoselective reduction of an extremely unreactive lactam in the presence of a readily reduced lactone.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Indole Alkaloids / chemical synthesis*
  • Indole Alkaloids / chemistry
  • Molecular Structure
  • Stereoisomerism

Substances

  • Indole Alkaloids
  • scholarisine A