A Total Synthesis of (±)-Leuconodines D and E

J Org Chem. 2019 Nov 1;84(21):13890-13896. doi: 10.1021/acs.joc.9b02054. Epub 2019 Oct 2.

Abstract

A new synthetic route for a short synthesis of (±)-leuconodines D and E was developed. The rapid construction of the diaza[5.5.6.6]fenestrane core was achieved through a sequence involving a Pd-catalyzed aerobic oxidative Heck cross-coupling reaction for the construction of indole δ-lactam containing a full-carbon quaternary center, an epoxidative cyclization for the assembly of pyrroloindole, and a ring-closing metathesis for the construction of the piperidine ring. As a result, the total synthesis of (±)-leuconodine E (2) was achieved for the first time within a 10-step linear sequence, and a more concise total synthesis of (±)-leuconodine D (1) was accomplished within a 12-step linear sequence from the commercially available tryptophol.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chemistry Techniques, Synthetic
  • Indole Alkaloids / chemical synthesis*
  • Indole Alkaloids / chemistry*
  • Models, Molecular
  • Molecular Conformation

Substances

  • Indole Alkaloids