Modular access to complex prodiginines: total synthesis of (+)-roseophilin via its 2-azafulvene prototropisomer

J Am Chem Soc. 2013 Mar 13;135(10):3788-91. doi: 10.1021/ja400473v. Epub 2013 Mar 1.

Abstract

Ansa-bridged prodiginines are bioactive pigments produced by bacteria. Certain of these structures are reported to be antagonists of protein-protein interactions involved in apoptosis. We describe a new entry to alkaloids of this type, demonstrated with a concise asymmetric synthesis of (+)-roseophilin (3). Our route constructs the pyrrolophane motif via phosphoryl transfer-terminated macroaldolization and passes through a previously unexplored prototropic form of the natural product.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aza Compounds / chemistry*
  • Cyclopentanes / chemistry*
  • Heterocyclic Compounds, 3-Ring / chemical synthesis
  • Heterocyclic Compounds, 3-Ring / chemistry
  • Molecular Structure
  • Pyrroles / chemical synthesis
  • Pyrroles / chemistry
  • Stereoisomerism

Substances

  • 2-azafulvene
  • Aza Compounds
  • Cyclopentanes
  • Heterocyclic Compounds, 3-Ring
  • Pyrroles
  • roseophilin