Copper-catalyzed asymmetric 1,6-conjugate addition of in situ generated para-quinone methides with β-ketoesters

Chem Commun (Camb). 2022 Jun 8;58(46):6653-6656. doi: 10.1039/d2cc00146b.

Abstract

A Cu-catalyzed asymmetric 1,6-conjugate addition of in situ generated para-quinone methides (p-QMs) with β-ketoester has been developed to construct a ketoester skeleton bearing an adjacent tertiary-quaternary carbon stereocenter in good yields and high enantioselectivities. This is the first example of metal-catalyzed asymmetric transformations of the in situ generated p-QMs, avoiding using pre-synthesized p-QMs requiring bulky 2,6-substitutions and highlighting a new dual catalytic activation with the chiral bis(oxazoline)-metal complex acting as a normal Lewis acid to activate the β-ketoesters and a source of Brønsted acid responsible for generating the p-QMs in situ.

MeSH terms

  • Catalysis
  • Copper*
  • Indolequinones*
  • Metals

Substances

  • Indolequinones
  • Metals
  • quinone methide
  • Copper