Synthesis of tertiary arylamines: Lewis acid-catalyzed direct reductive N-alkylation of secondary amines with ketones through an alternative pathway

Chem Commun (Camb). 2016 Aug 11;52(62):9648-51. doi: 10.1039/c6cc04381j. Epub 2016 Jul 1.

Abstract

We report herein a highly efficient, tin(ii)/PMHS catalyzed reductive N-alkylation of arylamines with ketones affording tertiary arylamines. A very wide substrate scope was observed for the current catalytic method as all six permutations of ketones/aldehydes/heterocyclic carbonyls and primary/secondary/heterocyclic amines were well tolerated, enabling access to secondary, tertiary and heterocyclic amines. The method is also convenient for the synthesis of N-substituted isoindolinones and phthalazinones via a tandem amination-amidation sequence. Mechanistic investigations revealed a carbocationic pathway instead of an ordinary direct reductive amination pathway.

MeSH terms

  • Alkylation
  • Amines / chemical synthesis*
  • Amines / chemistry*
  • Catalysis
  • Ketones / chemistry*
  • Lewis Acids / chemistry*
  • Molecular Structure

Substances

  • Amines
  • Ketones
  • Lewis Acids