Improved synthesis of C4α- and C4β-methyl analogues of 2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylate

Org Lett. 2012 Jun 1;14(11):2662-5. doi: 10.1021/ol300516y. Epub 2012 May 21.

Abstract

An efficient and divergent synthesis of C4α- and C4β-methyl-substituted analogues of 2-aminobicyclo[3.1.0]hexane 2,6-dicarboxylate, which are important tools in the study of metabotropic glutamate receptor function, has been achieved. By taking advantage of an unanticipated facial selectivity of the bicyclo[3.1.0]hexane ring system, either the C4α- or C4β-methyl substituent was introduced in a highly stereoselective and high-yielding manner.

MeSH terms

  • Amino Acids, Cyclic / chemical synthesis*
  • Amino Acids, Cyclic / chemistry
  • Dicarboxylic Acids / chemical synthesis*
  • Dicarboxylic Acids / chemistry
  • Hexanes / chemistry*
  • Humans
  • Molecular Structure
  • Receptors, Metabotropic Glutamate / agonists
  • Receptors, Metabotropic Glutamate / physiology
  • Stereoisomerism

Substances

  • 2-aminobicyclo(3.1.0)hexane-2,6-dicarboxylate
  • Amino Acids, Cyclic
  • Dicarboxylic Acids
  • Hexanes
  • Receptors, Metabotropic Glutamate
  • n-hexane