General catalytic methylation of amines with formic acid under mild reaction conditions

Iván Sorribes, Kathrin Junge, Matthias Beller

Research output: Contribution to journalArticlepeer-review

99 Scopus citations

Abstract

A general catalytic protocol for the methylation of amines has been developed applying, for the first time, formic acid as the C1 building block and silanes as reducing agents. A broad range of aromatic and aliphatic, both primary and secondary, amines has been converted to the corresponding tertiary amines including [N-13C]-labelled drugs in good to excellent yields under mild conditions. Methylation made easy: A general catalytic protocol for the methylation of amines has been developed applying, for the first time, formic acid as the C1 building block and silanes as reducing agents. A broad range of aromatic and aliphatic, both primary and secondary, amines has been converted to the corresponding tertiary amines, including [N-13C]-labelled drugs, in good to excellent yields at mild conditions (see scheme; dppp=(1,3-bis(diphenylphosphino)propane)).

Original languageEnglish
Pages (from-to)7878-7883
Number of pages6
JournalChemistry - A European Journal
Volume20
Issue number26
DOIs
StatePublished - 23 Jun 2014
Externally publishedYes

Keywords

  • formic acid
  • homogeneous catalysis
  • methylation
  • platinum
  • silanes

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