Enantioselective reduction of ketoimines promoted by easily available (S)-proline derivatives

Beilstein J Org Chem. 2013 Apr 2:9:633-40. doi: 10.3762/bjoc.9.71. Print 2013.

Abstract

The behavior of readily synthesized and even commercially available (S)-proline derivatives, was studied in the trichlorosilane-mediated reduction of ketoimines. A small library of structurally and electronically modified chiral Lewis bases was considered; such compounds were shown to promote the enantioselective reduction of different substrates in good chemical yields. In the HSiCl3 addition to the model substrate N-phenylacetophenone imine, the organocatalyst of choice led to the formation of the corresponding amine with good stereoselectivity, up to 75% ee. Theoretical studies were also performed in order to elucidate the origin of the stereoselection.

Keywords: Lewis bases; chiral prolines; imine reduction; organocatalysis; trichlorosilane.