Step-economical access to valuable Weinreb amide 2,5-disubstituted pyrrolidines by a sequential one-pot two-directional cross-metathesis/cyclizing aza-Michael process

J Org Chem. 2013 Mar 15;78(6):2346-54. doi: 10.1021/jo302435a. Epub 2013 Feb 21.

Abstract

Double cross-metathesis of 1,5-hexadiene with a variety of electron-deficient alkenes including the reluctant Weinreb acrylamide has been successfully accomplished. It was found that the process is quite general, and microwave irradiation effectively accelerates cross-coupling metathesis. This promotes a very versatile and high yielding methodology for the synthesis of symmetric Michael acceptors, which can be transformed into 2,5-disubstituted pyrrolidines through a sequential one-pot two-directional cross-metathesis/ring-closing double aza-Michael process.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylamides / chemistry*
  • Alkenes / chemistry*
  • Catalysis
  • Cross-Linking Reagents / chemistry*
  • Cyclization
  • Microwaves
  • Molecular Structure
  • Pyrrolidines / chemical synthesis*
  • Pyrrolidines / chemistry*
  • Stereoisomerism

Substances

  • Acrylamides
  • Alkenes
  • Cross-Linking Reagents
  • Pyrrolidines