Functionalized Polyhydroquinolines from Amino Acids Using a Key One-Pot Cyclization Cascade and Application to the Synthesis of (±)-Δ7-Mesembrenone

Org Lett. 2021 Nov 5;23(21):8606-8611. doi: 10.1021/acs.orglett.1c03323. Epub 2021 Oct 25.

Abstract

Substituted polyhydroquinolines are ubiquitous skeletal cores found in drugs and bioactive natural products. As a new route to access this motif, we successfully developed a one-pot cyclization cascade with high chemocontrol and diastereoselectivity. The sequence generates two cycles, three carbon-carbon bonds, and an all-carbon quaternary center in a highly convergent process. Functionalized polyhydroquinolines and congeners can be accessed from commercially available amino acids. This versatile and robust strategy was applied to the synthesis of (±)-Δ7-mesembrenone.

MeSH terms

  • Amino Acids* / chemical synthesis
  • Amino Acids* / chemistry
  • Cyclization
  • Molecular Structure
  • Quinolines* / chemical synthesis
  • Quinolines* / chemistry
  • Stereoisomerism

Substances

  • Amino Acids
  • Quinolines