Construction of Chiral Isotetronic Acid-Fused Thiochromane via Doubly Annulative Strategy

J Org Chem. 2021 Mar 19;86(6):4448-4456. doi: 10.1021/acs.joc.0c02878. Epub 2021 Mar 2.

Abstract

A sulfa-Michael/aldol/lactonization cascade reaction has been established to construct isotetronic acid-fused thiochromanes in a highly stereoselective fashion (≥11:1 dr, 35-98% ee). The tricyclic products were obtained in 35-99% isolated yields in the presence of a bifunctional squaramide. Three reactive sites of β,γ-unsaturated α-ketoester, including the less-explored ester carbonyl group, were sequentially utilized to construct two fused heterocycles in a one-pot operation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Esters*
  • Stereoisomerism

Substances

  • Esters