Chiral O-(Z-alpha-aminoacyl) sugars: convenient building blocks for glycopeptide libraries

Bioconjug Chem. 2007 May-Jun;18(3):994-8. doi: 10.1021/bc0603687. Epub 2007 Apr 19.

Abstract

1,2:3,4-Di-O-isopropylidene-alpha-D-galactopyranose (2), 1,2:5,6-di-O-isopropylidene-d-glucose (5), and 2,3:5,6-di-O-isopropylidene-alpha-D-mannofuranose (7) are efficiently O-acylated in 78-96% yields with readily available N-(Z-alpha-aminoacyl)benzotriazoles 1a-e, 1d+1d' under microwave irradiation to give chiral 3a-d, 4, 6a-d, 8a,b and diastereomeric mixtures (3d+3d'), (6a+6a'), and (6d+6d'). The original chirality was retained as evidenced by HPLC. The diisopropylidene protecting groups were removed from compounds 3a,d, 6d to give the free O-(Z-alpha-aminoacyl) sugars 9a,b, 10.

MeSH terms

  • Carbamates / chemical synthesis
  • Carbamates / chemistry*
  • Glycopeptides / chemical synthesis
  • Glycopeptides / chemistry*
  • Hexoses / chemical synthesis
  • Hexoses / chemistry*
  • Peptide Library*
  • Stereoisomerism

Substances

  • (3,4,5,6-tetrahydroxytetrahydro-2H-pyran-2-yl)methyl 2-((benzyloxy)carbonyl)amino-3-phenylpropanoate
  • Carbamates
  • Glycopeptides
  • Hexoses
  • Peptide Library