An investigation into the electrophilic cyclisation of N-acyl-pyrrolidinium ions: a facile synthesis of pyrrolo-tetrahydroisoquinolones and pyrrolo-benzazepinones

Org Biomol Chem. 2009 Sep 7;7(17):3561-71. doi: 10.1039/b907400g. Epub 2009 Jul 9.

Abstract

The triflic acid-mediated cyclisation of N-arylmethyl- and N-arylethyl-acylpyrrolidinium ions gave moderate to good yields of pyrrolo-tetrahydroisoquinolones and pyrrolo-benzazepinones respectively. Electron-donating R substituents enhanced the rate of reaction and gave higher yields than electron-withdrawing substituents. Substituents on the methyl or ethyl chain in general enhanced the reaction, unless sterically encumbered. The equivalent acylpiperidinium ions cyclised much slower and in lower yield.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzazepines / chemical synthesis*
  • Cyclization
  • Isoquinolines / chemical synthesis*
  • Kinetics
  • Pyrrolidines / chemistry*

Substances

  • Benzazepines
  • Isoquinolines
  • Pyrrolidines
  • pyrrolidine