Organocatalytic Asymmetric Synthesis of Biologically Relevant 3,3- Dihydroxyphenyloxindoles via para-Quinone Methides Derived from Isatins

J Org Chem. 2021 Apr 16;86(8):5489-5498. doi: 10.1021/acs.joc.0c03004. Epub 2021 Mar 29.

Abstract

The first asymmetric synthetic approach to biologically relevant 3,3-diphenyloloxindoles was developed using para-quinone methides derived from isatins and phenols. Chiral phosphoric acid efficiently catalyzed the reaction and delivered 3,3-diphenyloloxindoles under mild conditions with up to an equivalent yield and excellent enantioselectivity (up to >99% ee). The chirality was maintained in further synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Indolequinones*
  • Isatin*
  • Stereoisomerism

Substances

  • Indolequinones
  • quinone methide
  • Isatin