Bifunctional asymmetric catalysis: amplification of Brønsted basicity can orthogonally increase the reactivity of a chiral Brønsted acid

J Am Chem Soc. 2010 Mar 10;132(9):2880-2. doi: 10.1021/ja908814h.

Abstract

The reactivity of a series of symmetrical chiral Brønsted acids (polar ionic hydrogen-bond donors) follows the counterintuitive trend wherein the more Brønsted basic member is a more effective catalyst for the aza-Henry (nitro-Mannich) reaction. This new design element leads to a substantially more reactive catalyst for the aza-Henry reaction, one that can promote the addition of a secondary nitroalkane. Additionally, when an achiral Brønsted acid (TfOH) is used in slight excess of the neutral, chiral bisamidine ligand, diastereoselection can be optimized to levels generally greater than 15:1 while the enantioselection remains unchanged at generally >90% ee.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Acids / chemistry*
  • Amidines / chemistry*
  • Aza Compounds / chemical synthesis*
  • Aza Compounds / chemistry
  • Catalysis
  • Molecular Structure
  • Stereoisomerism

Substances

  • Acids
  • Amidines
  • Aza Compounds