A practical new chiral controller for asymmetric Diels-Alder and alkylation reactions

Org Lett. 1999 Dec 2;1(11):1741-4. doi: 10.1021/ol991007s.

Abstract

[formula: see text] The enantiomerically pure hydroxy sulfones (+)- and (-)-2 have been prepared from 1,2-epoxycyclohexane by a simple and practical procedure. The acrylate esters of these alcohols undergo BCl3-catalyzed Diels-Alder reactions with a variety of dienes at -78 to -55 degrees C in CH2Cl2 or C7H8 with high dienophile face selectivity (Table 1). The chiral esters so formed are readily cleaved with recovery of the controllers (+)- or (-)-2. Esters of (+)- and (-)-2 can be converted to Z-potassium enolates and alkylated with high face selectivity.

Publication types

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

MeSH terms

  • Alkylation
  • Crystallography, X-Ray
  • Cyclization
  • Stereoisomerism
  • Sulfones / chemical synthesis*

Substances

  • Sulfones