First highly enantioselective synthesis of benzodiazepinones by catalytic hydrogenation

Magnus Rueping*, Estíbaliz Merino, René M. Koenigs

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

65 Scopus citations


The first catalytic enantioselective synthesis of benzodiazepinones employing an efficient hydrogenation protocol has been developed. The corresponding products are obtained in good yields, with excellent enantioselectivities and broad functional group tolerance. In addition, a one-pot procedure involving in situ generation of benzodiazepin-2-ones followed by asymmetric reduction is presented.

Original languageEnglish (US)
Pages (from-to)2629-2634
Number of pages6
JournalAdvanced Synthesis and Catalysis
Issue number14-15
StatePublished - Oct 4 2010
Externally publishedYes


  • Brønsted acids
  • Hantzsch dihydropyridines
  • asymmetric hydrogenation
  • enantioselective reduction
  • organocatalysis
  • β-amino acids

ASJC Scopus subject areas

  • Catalysis
  • Organic Chemistry


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