Using Neighboring-Group Participation for Acyclic Stereocontrol in Diastereoselective Substitution Reactions of Acetals

Org Lett. 2020 Jun 5;22(11):4113-4117. doi: 10.1021/acs.orglett.0c01166. Epub 2020 May 11.

Abstract

Neighboring-group participation of an ester enabled stereocontrol in substitution reactions of acyclic acetals. The ester group formed a trans-fused dioxolenium ion intermediate, which underwent a substitution reaction at the acetal carbon atom to afford the product with high diastereoselectivity. Neighboring-group participation was confirmed by isolating dioxolane products resulting from nucleophilic addition at C-2 of a 1,3-dioxolenium ion intermediate. Using a pivaloate ester as the participating group in combination with strong nucleophiles produced substitution products with diastereoselectivities of ≥90:10.

Publication types

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

MeSH terms

  • Acetals / chemistry*
  • Aldehydes / chemical synthesis*
  • Aldehydes / chemistry
  • Esters / chemistry*
  • Molecular Structure
  • Stereoisomerism

Substances

  • Acetals
  • Aldehydes
  • Esters