3-Alkenyl-2-silyloxyindoles in vinylogous Mannich reactions: synthesis of aminated indole-based scaffolds and products

Org Lett. 2014 Feb 7;16(3):932-5. doi: 10.1021/ol4036598. Epub 2014 Jan 16.

Abstract

The first Lewis acid catalyzed vinylogous Mukaiyama-type Mannich addition of 3-alkenyl-2-silyloxyindoles to in situ generated N-Boc imines has been established, which affords chiral α-alkylidene-δ-amino-2-oxindole products with good efficiency and complete γ-site- and Z-selectivity. The reaction is wide in scope, as it can be applied with equal convenience to different silyloxyindole donors and aromatic or aliphatic aminal-derived aldimine acceptors. The utility of these scaffolds is demonstrated by their easy transformation into either spirocyclopropane oxindole or homotryptamine-like products, featuring nontraditional indole-based skeleton connections.

MeSH terms

  • Alkenes / chemistry*
  • Catalysis
  • Indoles / chemistry*
  • Lewis Acids / chemistry*
  • Molecular Structure
  • Oxindoles
  • Silanes / chemistry*
  • Stereoisomerism

Substances

  • Alkenes
  • Indoles
  • Lewis Acids
  • Oxindoles
  • Silanes
  • 2-oxindole
  • indole