Remote Enantioselective [4 + 1] Annulation with Copper-Vinylvinylidene Intermediates

J Am Chem Soc. 2022 Nov 23;144(46):21347-21355. doi: 10.1021/jacs.2c09572. Epub 2022 Nov 11.

Abstract

The first copper-catalyzed enantioselective [4 + 1] annulation of yne-allylic esters with 1,3-dicarbonyl compounds was realized through an elegant remote stereocontrol strategy. The very remote ε regioselective nucleophilic substitution was developed by employing a novel chiral copper-vinylvinylidene species from the new C4 synthon yne-allylic esters. Thus, greatly diverse spirocycles were obtained with ample scope and excellent levels of chemo-, regio-, and enantioselectivities. Moreover, detailed mechanistic studies suggest an yne-allylic substitution and Conia-ene cascade pathway on the remote stereochemical induction progress.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Copper* / chemistry
  • Esters*
  • Molecular Structure
  • Stereoisomerism

Substances

  • Copper
  • Esters