Catalytic asymmetric inverse-electron-demand aza-Diels-Alder reaction of 1,3-diazadienes with 3-vinylindoles

Chem Commun (Camb). 2022 Jul 5;58(54):7515-7518. doi: 10.1039/d2cc02458f.

Abstract

A facile chiral phosphoric-acid catalyzed asymmetric inverse-electron-demand aza-Diels-Alder reaction of 1,3-diazadienes with 3-vinylindoles was established. By using this mild and practical protocol, a broad range of benzothiazolopyrimidines with three contiguous stereogenic centers were prepared in good yields and excellent diastereo- and enantio-selectivities (43 examples, up to 83% yield, >99% ee and all >20 : 1 dr). A plausible concerted reaction pathway enabled by the dual hydrogen-bonding effect was proposed to account for the observed excellent enantioselectivity and specific trans-trans diastereoselectivity.

MeSH terms

  • Alkenes
  • Aza Compounds
  • Catalysis
  • Cycloaddition Reaction
  • Electrons*
  • Stereoisomerism

Substances

  • 1,3-diazadiene
  • Alkenes
  • Aza Compounds