Lewis acid catalyzed cyclization of glycals/2-deoxy-D-ribose with arylamines: additional findings on product structure and reaction diastereoselectivity

J Org Chem. 2011 Nov 4;76(21):8833-9. doi: 10.1021/jo2015483. Epub 2011 Oct 7.

Abstract

The cyclization reactions of arylamines with 2-deoxy-D-ribose or glycals were reinvestigated in the current report. In the montmorillonite KSF- or InCl(3)-initiated reactions of 2-deoxy-D-ribose with arylamines, a pair of diastereomeric tetrahydro-2H-pyran-fused tetrahydroquinolines was obtained in a nearly 1:1 ratio where the structure of one diastereomer was incorrectly assigned in the literature. Meanwhile, the diastereoselectivity in InBr(3)-catalyzed cyclization of glycals with arylamines was also incorrectly reported previously. It was found that high diastereomeric selectivity was achieved only when a C5-substituted glycal was used; otherwise, a pair of diastereomers was obtained in moderate yield with 1:1 diastereomeric ratio. Furthermore, tetrahydrofuran-fused tetrahydroquinolines 5b and 5b' were also prepared successfully by using TBDPS-protected ribose as the glycal precursor and montmorillonite KSF as the activator.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amines / chemistry*
  • Bentonite / chemistry*
  • Catalysis
  • Cyclization
  • Furans / chemistry
  • Lewis Acids / chemistry*
  • Molecular Structure
  • Quinolines / chemistry
  • Ribose / chemistry*
  • Stereoisomerism

Substances

  • Amines
  • Furans
  • Lewis Acids
  • Quinolines
  • Bentonite
  • Ribose