Synthesis of cyclobutane serine analogues

J Org Chem. 2005 Jan 7;70(1):330-3. doi: 10.1021/jo048943s.

Abstract

In this paper, we describe a thermal [2 + 2] cycloaddition involving 2-acylaminoacrylates as electron-poor acceptor alkenes, a reaction that involves a Michael-Dieckmann-type process. The reaction gives rise to a new substituted cyclobutane skeleton that can be transformed into amino acid derivatives. For example, a number of transformations were carried out to give the two pairs of stereoisomers of the 2-hydroxycyclobutane-alpha-amino acid serine analogue (c(4)Ser); compounds 22 and 23. This synthesis covers a gap in knowledge in the broad field of restricted amino acids.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Cyclobutanes / chemical synthesis*
  • Cyclobutanes / chemistry
  • Indicators and Reagents
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Serine / analogs & derivatives*
  • Serine / chemical synthesis*
  • Stereoisomerism
  • Thermodynamics

Substances

  • Cyclobutanes
  • Indicators and Reagents
  • Serine