A one-pot cascade to protoberberine alkaloids via Stevens rearrangement of nitrile-stabilized ammonium ylides

J Org Chem. 2015 Feb 6;80(3):2010-6. doi: 10.1021/jo502842s. Epub 2015 Jan 27.

Abstract

A facile one-pot synthesis of protoberberines from readily accessible 1,2,3,4-tetrahydroisoquinoline-1-carbonitriles and 1,2-bis(bromomethyl)arenes is described. The reaction cascade comprises four consecutive transformations, all of which can be effected under a single set of conditions. Ten protoberberines, including the alkaloids pseudopalmatine and pseudoepiberberine, were prepared in yields up to 86% according to this strategy. No chromatographic purification of the products is required, and the route is devoid of any protecting group manipulations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / chemical synthesis*
  • Alkaloids / chemistry*
  • Ammonium Compounds / chemistry*
  • Berberine Alkaloids / chemical synthesis*
  • Berberine Alkaloids / chemistry*
  • Molecular Structure
  • Nitriles / chemistry*
  • Tetrahydroisoquinolines / chemistry*

Substances

  • Alkaloids
  • Ammonium Compounds
  • Berberine Alkaloids
  • Nitriles
  • Tetrahydroisoquinolines
  • protoberberine