Studies on the bisoxazoline- and (-)-sparteine-mediated enantioselective addition of organolithium reagents to imines

Scott E. Denmark, Noriyuki Nakajima, Cory M. Stiff, Olivier J.C. Nicaise, Michael Kranz

Research output: Contribution to journalArticlepeer-review

Abstract

The enantioselective addition of organolithium reagents to N-anisylaldimines promoted by chiral bisoxazolines and (-)-sparteine as external ligands is described. This reaction proceeds readily with a wide range of aldimine substrates (aliphatic, aromatic, olefinic) and organolithium nucleophiles (Me, n-Bu, Ph, vinyl) in excellent yields (81-99%) and with high enantioselectivities (up to 97:3.0 er). The external ligands can be used in substoichiometric amounts albeit with slightly attenuated enantioselectivities. A systematic evaluation of the structural features of the bisoxazolines revealed a primary contribution from the substituent at C(4) and a secondary influence from the bridging substituents. A computational analysis (PM3) provided a clear rationalization for the origin of enantioselectivity.

Original languageEnglish (US)
Pages (from-to)1023-1045
Number of pages23
JournalAdvanced Synthesis and Catalysis
Volume350
Issue number7-8
DOIs
StatePublished - May 5 2008

Keywords

  • Aldimines
  • Bisoxazolines
  • Catalysis
  • Enantioselective addition
  • Organolithium reagents

ASJC Scopus subject areas

  • Catalysis
  • Organic Chemistry

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