Solvent-free cross-dehydrogenative coupling reactions under high speed ball-milling conditions applied to the synthesis of functionalized tetrahydroisoquinolines

J Org Chem. 2011 Nov 4;76(21):9144-50. doi: 10.1021/jo2015533. Epub 2011 Oct 12.

Abstract

Solvent-free reaction using a high-speed ball milling technique has been first applied to cross-dehydrogenative coupling (CDC) reactions between tetrahydroisoquinolines and three types of pronucleophiles such as nitroalkanes, alkynes, and indoles. All coupling products were obtained in good yields at short reaction times (no more than 40 min). When alkynes and indoles were used as pronucleophile, the reactions can be catalyzed efficiently by recoverable copper balls without any additional metal catalyst.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Copper / chemistry
  • Cross-Linking Reagents / chemistry*
  • Molecular Structure
  • Nitro Compounds / chemistry
  • Solvents / chemistry*
  • Tetrahydroisoquinolines / chemical synthesis*
  • Tetrahydroisoquinolines / chemistry*

Substances

  • Cross-Linking Reagents
  • Nitro Compounds
  • Solvents
  • Tetrahydroisoquinolines
  • Copper