Asymmetric synthesis of orthogonally protected trans-cyclopropane gamma-amino acids via intramolecular ring closure

Org Biomol Chem. 2006 Aug 21;4(16):3113-6. doi: 10.1039/b606879k. Epub 2006 Jul 6.

Abstract

The synthesis of enantiomerically-enriched trans-cyclopropane amino- and hydroxy-acids can be achieved by intramolecular ring closure in moderate to good yields. The optically active cyclopropane precursors are easily prepared in a short sequence from inexpensive, commercially available olefins and tert-butyl acetate. Several leaving groups and bases were compared for the cyclopropanation step, showing that the diphenylphosphinate and tosyl leaving groups give the best results when used in combination with either LDA or NaHMDS.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acids / chemical synthesis*
  • Amino Acids / chemistry
  • Cyclization
  • Cyclopropanes / chemistry*

Substances

  • Amino Acids
  • Cyclopropanes
  • cyclopropane