Synthesis of 3-benzylisoquinolines by domino imination/cycloisomerisation of 2-propargylbenzaldehydes

Org Biomol Chem. 2014 Oct 28;12(40):8019-30. doi: 10.1039/c4ob01583e. Epub 2014 Sep 19.

Abstract

An easy entry to uncommon 2-propargylbenzaldehydes was developed. 2-Propargylbenzaldehydes demonstrated to be suitable building blocks for the synthesis of 3-benzyl isoquinolines by microwave promoted domino imination/cycloisomerisation in the presence of ammonium acetate. A small library of 3-benzyl isoquinolines was obtained in good yields under mild reaction conditions. Two alternative plausible reaction mechanisms are proposed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzaldehydes / chemistry*
  • Benzylisoquinolines / chemical synthesis*
  • Benzylisoquinolines / chemistry
  • Cyclization
  • Imines / chemistry*
  • Molecular Structure

Substances

  • Benzaldehydes
  • Benzylisoquinolines
  • Imines