Expeditious and Divergent Total Syntheses of Aspidosperma Alkaloids Exploiting Iridium(I)-Catalyzed Generation of Reactive Enamine Intermediates

Angew Chem Int Ed Engl. 2016 Oct 17;55(43):13436-13440. doi: 10.1002/anie.201605503. Epub 2016 Sep 23.

Abstract

A new approach for the divergent total syntheses of (±)-vincaminorine, (±)-N-methylquebrachamine, (±)-quebrachamine, (±)-minovine and (±)-vincadifformine, each in less than 10 linear steps starting from a single δ-lactam building block, is reported. Key to our route design is the late-stage generation of reactive enamine functionality from stable indole-linked δ-lactams via a highly chemoselective iridium(I)-catalyzed reduction. The efficiently formed secodine intermediates subsequently undergo either a formal Diels-Alder cycloaddition or a competitive Michael addition/reduction to access aspidosperma-type alkaloids in excellent diastereoselectivities. Product selectivity could be controlled by changing the indole N-protecting group in the reductive cyclization precursors. An asymmetric variant of this synthetic strategy for the synthesis of (+)-20-epi-ibophyllidine is also described.

Keywords: aspidosperma alkaloid; enamine; iridium catalyzed reduction; lactam; total synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / chemical synthesis*
  • Alkaloids / chemistry
  • Amines / chemical synthesis
  • Amines / chemistry*
  • Aspidosperma / chemistry*
  • Catalysis
  • Cycloaddition Reaction
  • Iridium / chemistry*
  • Molecular Structure

Substances

  • Alkaloids
  • Amines
  • Iridium